Article(id=1220655524194992260, tenantId=1146029695717560320, journalId=1189982191388893191, issueId=1220655523473571972, articleNumber=null, orderNo=null, doi=10.16438/j.0513-4870.2020-0182, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=research-article, receivedDate=1582646400000, receivedDateStr=2020-02-26, revisedDate=null, revisedDateStr=null, acceptedDate=1583942400000, acceptedDateStr=2020-03-12, onlineDate=1768956555651, onlineDateStr=2026-01-21, pubDate=1597161600000, pubDateStr=2020-08-12, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1768956555651, onlineIssueDateStr=2026-01-21, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1768956555651, creator=13701087609, updateTime=1768956555651, updator=13701087609, issue=Issue{id=1220655523473571972, tenantId=1146029695717560320, journalId=1189982191388893191, year='2020', volume='55', issue='8', pageStart='1707', pageEnd='1982', issueExtLink='null', onlineDate='null', pubDate='null', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1768956555479, creator=13701087609, updateTime=1768986579152, updator=13701087609, preIssue=null, nextIssue=null, ext={EN=IssueExt(id=1220781451944051235, tenantId=1146029695717560320, journalId=1189982191388893191, issueId=1220655523473571972, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1220781451944051236, tenantId=1146029695717560320, journalId=1189982191388893191, issueId=1220655523473571972, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null}, startPage=1707, endPage=1725, ext={EN=ArticleExt(id=1220655524652171398, articleId=1220655524194992260, tenantId=1146029695717560320, journalId=1189982191388893191, language=EN, title=Examples of biology-driven drug design, columnId=1220655291499201388, journalTitle=Acta Pharmaceutica Sinica, columnName=Professionals Forums, runingTitle=null, highlight=null, articleAbstract=
Pharmacological activity and drug likeness depend in principle upon the microscopic structure and macroscopic properties of drugs, which reside in their molecular structures. By means of medicinal chemistry the evolution of an active compound to a novel drug (NME) essentially makes the two pillars coexistence in one chemical structure, which either could merge as an intrinsic structure or connect from external fragments to each other with covalent bonds. Since the new millennium the advance in biology provides several knowledge and technologies, for example humanized monoclonal antibody, proteasome-ubiquitin system, allosteric modulation, natural macromolecules, structural biology, etc., for innovation of novel medicines. Taking several examples on marketed drugs or drug candidates in clinical trials, this article tries to concisely illustrate R & D conception of biology-driven drug design.
, correspAuthors=Zong-ru GUO, authorNote=null, correspAuthorsNote=null, copyrightStatement=Copyright ©2020 Acta Pharmaceutica Sinica. All rights reserved., copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, authorCompany=null, fund=null, authors=null, authorsList=Zong-ru GUO), CN=ArticleExt(id=1220655530503225827, articleId=1220655524194992260, tenantId=1146029695717560320, journalId=1189982191388893191, language=CN, title=例解生物学驱动的药物设计, columnId=1190335349206389552, journalTitle=药学学报, columnName=专家论坛, runingTitle=null, highlight=null, articleAbstract=
药理活性和成药性原则上取决于药物的微观结构和宏观性质,这些都寓于分子结构之中。药物化学将活性化合物演化成药物,是将二者融合一起,优化而得。融合操作既可以是内在的结构体现,也可以是外在的片段连接。新世纪以来的生物学进展为此提供了许多切入点,例如人源化单克隆抗体、蛋白酶体-泛素系统、变构调节、天然大环化合物、结构生物学等。本文以上市的或处于临床试验的药物研发要点,尝试解析生物学驱动的研发理念。
, correspAuthors=郭宗儒, authorNote=null, correspAuthorsNote=
, copyrightStatement=版权所有©《药学学报》编辑部2020, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=Cn876WL27VN9GNDRHhIuug==, magXml=o41V+Xl2DXIoWcmDAee6hQ==, pdfUrl=null, pdf=8y/QNxthTaIb4FEAq587Kw==, pdfFileSize=2552001, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=ExFEmXxp7FgrlBrKqyHUOQ==, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=6VqeIk5K09GDjBd5+AnCrw==, mapNumber=null, authorCompany=null, fund=null, authors=null, authorsList=郭宗儒)}, authors=[Author(id=1220655530918461952, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, orderNo=0, firstName=null, middleName=null, lastName=null, nameCn=null, orcid=null, stid=null, country=null, authorPic=null, dead=0, email=zrguo@imm.ac.cn, emailSecond=null, emailThird=null, correspondingAuthor=1, authorType=1, ext={EN=AuthorExt(id=1220655530985570822, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, authorId=1220655530918461952, language=EN, stringName=Zong-ru GUO, firstName=Zong-ru, middleName=null, lastName=GUO, prefix=null, suffix=null, authorComment=null, nameInitials=null, affiliation=null, department=null, xref=
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Breslin HJ ,
Cai CZ ,
Miskowski TA et al . Identification of potent phenyl imidazoles as opioid receptor agonists[J].
Bioorg Med Chem Lett,
2006,
16: 2505-2508., articleTitle=Identification of potent phenyl imidazoles as opioid receptor agonists, refAbstract=null), Reference(id=1220655536643687233, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1016/j.coph.2013.11.006, pmid=null, pmcid=null, year=2014, volume=15, issue=null, pageStart=22, pageEnd=27, url=null, language=null, rfNumber=[2], rfOrder=1, authorNames=Sanguinetti MC, journalName=Curr Opin Pharmacol, refType=null, unstructuredReference=
Sanguinetti MC . HERG1 channel agonists and cardiac arrymthmia[J].
Curr Opin Pharmacol,
2014,
15: 22-27., articleTitle=HERG1 channel agonists and cardiac arrymthmia, refAbstract=null), Reference(id=1220655536735961926, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm001126+, pmid=null, pmcid=null, year=2002, volume=45, issue=null, pageStart=623, pageEnd=630, url=null, language=null, rfNumber=[3], rfOrder=2, authorNames=Singh BN, Malm J, Mellin C, journalName=J Med Chem, refType=null, unstructuredReference=
Singh BN ,
Malm J ,
Mellin C et al . Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone[J].
J Med Chem,
2002,
45: 623-630., articleTitle=Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone, refAbstract=null), Reference(id=1220655536819848014, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1124/mol.107.041152, pmid=null, pmcid=null, year=2008, volume=73, issue=null, pageStart=639, pageEnd=651, url=null, language=null, rfNumber=[4], rfOrder=3, authorNames=Gordon E, Lozinskaya IM, Lin Z, journalName=Mol Pharmacol, refType=null, unstructuredReference=
Gordon E ,
Lozinskaya IM ,
Lin Z et al . 2-[2-(3, 4-Dichloro-phenyl)-2, 3-dihydro-1
H-isoindol-5-ylamino]-nicotinic acid (PD-307243) causes instantaneous current through human ether-a-go-go-related gene potassium channels[J].
Mol Pharmacol,
2008,
73: 639-651., articleTitle=2-[2-(3, 4-Dichloro-phenyl)-2, 3-dihydro-1
H-isoindol-5-ylamino]-nicotinic acid (PD-307243) causes instantaneous current through human ether-a-go-go-related gene potassium channels, refAbstract=null), Reference(id=1220655536895345495, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1016/S0960-894X(99)00250-4, pmid=null, pmcid=null, year=1999, volume=9, issue=null, pageStart=1625, pageEnd=1630, url=null, language=null, rfNumber=[5], rfOrder=4, authorNames=Muller GW, Chen R, Huang SY, journalName=Bioorg Med Chem Lett, refType=null, unstructuredReference=
Muller GW ,
Chen R ,
Huang SY et al . Amino-substituted thalidomide analogs:potent inhibitors of TNF-alpha production[J].
Bioorg Med Chem Lett,
1999,
9: 1625-1630., articleTitle=Amino-substituted thalidomide analogs:potent inhibitors of TNF-alpha production, refAbstract=null), Reference(id=1220655537025368926, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.6b01921, pmid=null, pmcid=null, year=2018, volume=61, issue=null, pageStart=535, pageEnd=542, url=null, language=null, rfNumber=[6], rfOrder=5, authorNames=Matyskiela ME, Zhang WH, Man HW, journalName=J Med Chem, refType=null, unstructuredReference=
Matyskiela ME ,
Zhang WH ,
Man HW et al . A celebron modulator (CC-220) with improved degredation of Ikaros and Aiolos[J].
J Med Chem,
2018,
61: 535-542., articleTitle=A celebron modulator (CC-220) with improved degredation of Ikaros and Aiolos, refAbstract=null), Reference(id=1220655537130226534, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1002/cmdc.200600221, pmid=null, pmcid=null, year=2007, volume=2, issue=null, pageStart=58, pageEnd=61, url=null, language=null, rfNumber=[7], rfOrder=6, authorNames=Pan Z, Scheerens H, Li S, journalName=ChemMedChem, refType=null, unstructuredReference=
Pan Z ,
Scheerens H ,
Li S et al . Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase[J].
ChemMedChem,
2007,
2: 58-61., articleTitle=Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase, refAbstract=null), Reference(id=1220655537235084143, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1158/1078-0432.CCR-16-0463, pmid=null, pmcid=null, year=2017, volume=23, issue=null, pageStart=2831, pageEnd=2841, url=null, language=null, rfNumber=[8], rfOrder=7, authorNames=Herman SEM, Montraveta A, Niemann CU, journalName=Clin Cancer Res, refType=null, unstructuredReference=
Herman SEM ,
Montraveta A ,
Niemann CU et al . The Bruton tyrosine kinase (BTK) inhibitor acalabrutinib demonstrates potent on-target effects and efficacy in two mouse models of chronic lymphocytic leukemia[J].
Clin Cancer Res,
2017,
23: 2831-2841., articleTitle=The Bruton tyrosine kinase (BTK) inhibitor acalabrutinib demonstrates potent on-target effects and efficacy in two mouse models of chronic lymphocytic leukemia, refAbstract=null), Reference(id=1220655537335747446, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.9b00687, pmid=null, pmcid=null, year=2019, volume=62, issue=null, pageStart=7923, pageEnd=7940, url=null, language=null, rfNumber=[9], rfOrder=8, authorNames=Guo YH, Liu Y, Hu N, journalName=J Med Chem, refType=null, unstructuredReference=
Guo YH ,
Liu Y ,
Hu N et al . Discovery of zanubrutinib (BGB-3111), a novel, potent, and selective covalent inhibitor of Bruton's tyrosine kinase[J].
J Med Chem,
2019,
62: 7923-7940., articleTitle=Discovery of zanubrutinib (BGB-3111), a novel, potent, and selective covalent inhibitor of Bruton's tyrosine kinase, refAbstract=null), Reference(id=1220655537436410752, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm060077j, pmid=null, pmcid=null, year=2006, volume=49, issue=null, pageStart=2750, pageEnd=2757, url=null, language=null, rfNumber=[10], rfOrder=9, authorNames=Bogen SL, Arasappan A, Bennet F, journalName=J Med Chem, refType=null, unstructuredReference=
Bogen SL ,
Arasappan A ,
Bennet F et al . Discovery of SCH446211(SCH6):a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication[J].
J Med Chem,
2006,
49: 2750-2757., articleTitle=Discovery of SCH446211(SCH6):a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication, refAbstract=null), Reference(id=1220655537545462661, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1016/S0960-894X(98)00029-8, pmid=null, pmcid=null, year=1998, volume=8, issue=null, pageStart=333, pageEnd=338, url=null, language=null, rfNumber=[11], rfOrder=10, authorNames=Adams J, Behnke M, Chen S, journalName=Bioorg Med Chem Lett, refType=null, unstructuredReference=
Adams J ,
Behnke M ,
Chen S et al . Potent and selective inhibitors of the proteasome:dipeptidyl boronic acids[J].
Bioorg Med Chem Lett,
1998,
8: 333-338., articleTitle=Potent and selective inhibitors of the proteasome:dipeptidyl boronic acids, refAbstract=null), Reference(id=1220655537675486094, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm0603724, pmid=null, pmcid=null, year=2006, volume=49, issue=null, pageStart=4447, pageEnd=4450, url=null, language=null, rfNumber=[12], rfOrder=11, authorNames=Baker SJ, Zhang YK, Akama T, journalName=J Med Chem, refType=null, unstructuredReference=
Baker SJ ,
Zhang YK ,
Akama T et al . Discovery of a new boron-containing antifungal agent, 5-fluoro-1, 3-dihydro-1-hydroxy-2, 1-benzoxaborole (AN2690), for the potential treatment of onychomycosis[J].
J Med Chem,
2006,
49: 4447-4450., articleTitle=Discovery of a new boron-containing antifungal agent, 5-fluoro-1, 3-dihydro-1-hydroxy-2, 1-benzoxaborole (AN2690), for the potential treatment of onychomycosis, refAbstract=null), Reference(id=1220655537780343702, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1016/j.bmcl.2009.03.007, pmid=null, pmcid=null, year=2009, volume=19, issue=null, pageStart=2129, pageEnd=2132, url=null, language=null, rfNumber=[13], rfOrder=12, authorNames=Akama T, Baker SJ, Zhang YK, journalName=Bioorg Med Chem Lett, refType=null, unstructuredReference=
Akama T ,
Baker SJ ,
Zhang YK et al . Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis[J].
Bioorg Med Chem Lett,
2009,
19: 2129-2132., articleTitle=Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis, refAbstract=null), Reference(id=1220655537872618399, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=null, pmid=null, pmcid=null, year=2017, volume=23, issue=null, pageStart=321, pageEnd=326, url=null, language=null, rfNumber=[14], rfOrder=13, authorNames=Metcalf B, Chuang C, Dufu K, journalName=ACS Med Chem Lett, refType=null, unstructuredReference=
Metcalf B ,
Chuang C ,
Dufu K et al . Discovery of GBT440, an orally bioavailable Rstate stabilizer of sickle cell hemoglobin[J].
ACS Med Chem Lett,
2017,
23: 321-326., articleTitle=Discovery of GBT440, an orally bioavailable Rstate stabilizer of sickle cell hemoglobin, refAbstract=null), Reference(id=1220655537969087403, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1016/j.bmc.2010.08.026, pmid=null, pmcid=null, year=2010, volume=18, issue=null, pageStart=6977, pageEnd=6986, url=null, language=null, rfNumber=[15], rfOrder=14, authorNames=Manley P, Stiefl N, Cowan-Jacob S, journalName=Bioorg Med Chem, refType=null, unstructuredReference=
Manley P ,
Stiefl N ,
Cowan-Jacob S et al . Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib[J].
Bioorg Med Chem,
2010,
18: 6977-6986., articleTitle=Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib, refAbstract=null), Reference(id=1220655538099110834, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm100395q, pmid=null, pmcid=null, year=2010, volume=53, issue=null, pageStart=4701, pageEnd=4719, url=null, language=null, rfNumber=[16], rfOrder=15, authorNames=Huang WS, Metcalf CA, Sundaramoorthi R, journalName=J Med Chem, refType=null, unstructuredReference=
Huang WS ,
Metcalf CA ,
Sundaramoorthi R et al . Discovery of 3-[2-(imidazo[1, 2-b]pyridazin-3-yl)ethynyl]-4-methyl-
N-{4-[(4-methylpiperazin-1-yl)-methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant[J].
J Med Chem,
2010,
53: 4701-4719., articleTitle=Discovery of 3-[2-(imidazo[1, 2-b]pyridazin-3-yl)ethynyl]-4-methyl-
N-{4-[(4-methylpiperazin-1-yl)-methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant, refAbstract=null), Reference(id=1220655538220745662, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm301581y, pmid=null, pmcid=null, year=2013, volume=56, issue=null, pageStart=879, pageEnd=894, url=null, language=null, rfNumber=[17], rfOrder=16, authorNames=Ren XM, Pan XF, Zhang Z, journalName=J Med Chem, refType=null, unstructuredReference=
Ren XM ,
Pan XF ,
Zhang Z et al . Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinihem[J].
J Med Chem,
2013,
56: 879-894., articleTitle=Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinihem, refAbstract=null), Reference(id=1220655538359157705, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1038/s41586-019-1694-1, pmid=null, pmcid=null, year=2019, volume=575, issue=null, pageStart=217, pageEnd=223, url=null, language=null, rfNumber=[18], rfOrder=17, authorNames=Canon J, Rex K, Saili AY, journalName=Nature, refType=null, unstructuredReference=
Canon J ,
Rex K ,
Saili AY et al . The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity[J].
Nature,
2019,
575: 217-223., articleTitle=The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity, refAbstract=null), Reference(id=1220655538480792536, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.9b01180, pmid=null, pmcid=null, year=2020, volume=63, issue=null, pageStart=52, pageEnd=65, url=null, language=null, rfNumber=[19], rfOrder=18, authorNames=Lanman BA, Allen JR, Allen JG, journalName=J Med Chem, refType=null, unstructuredReference=
Lanman BA ,
Allen JR ,
Allen JG et al . Discovery of a covalent inhibitor of KRASG12C (AMG 510) for the treatment of solid tumors[J].
J Med Chem,
2020,
63: 52-65., articleTitle=Discovery of a covalent inhibitor of KRASG12C (AMG 510) for the treatment of solid tumors, refAbstract=null), Reference(id=1220655538581455840, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1038/nature21702, pmid=null, pmcid=null, year=2017, volume=543, issue=null, pageStart=733, pageEnd=737, url=null, language=null, rfNumber=[20], rfOrder=19, authorNames=Wylie AA, Schoepfer J, Jahnke W, journalName=Nature, refType=null, unstructuredReference=
Wylie AA ,
Schoepfer J ,
Jahnke W et al . The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1[J].
Nature,
2017,
543: 733-737., articleTitle=The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1, refAbstract=null), Reference(id=1220655538682119146, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.8b01040, pmid=null, pmcid=null, year=2018, volume=61, issue=null, pageStart=8120, pageEnd=8135, url=null, language=null, rfNumber=[21], rfOrder=20, authorNames=Schoepfer J, Jahnke W, Berellini G, journalName=J Med Chem, refType=null, unstructuredReference=
Schoepfer J ,
Jahnke W ,
Berellini G et al . Discovery of asciminib (ABL001), an allosteric inhibitor of the tyrosine kinase activity of BCR-ABL1[J].
J Med Chem,
2018,
61: 8120-8135., articleTitle=Discovery of asciminib (ABL001), an allosteric inhibitor of the tyrosine kinase activity of BCR-ABL1, refAbstract=null), Reference(id=1220655538795365365, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.2174/092986709787315522, pmid=null, pmcid=null, year=2009, volume=16, issue=null, pageStart=455, pageEnd=472, url=null, language=null, rfNumber=[22], rfOrder=21, authorNames=Veleiro AS, Burton G, journalName=Curr Med Chem, refType=null, unstructuredReference=
Veleiro AS ,
Burton G . Structure-activity relationships of neuroactive steroids acting on the GABAA receptor[J].
Curr Med Chem,
2009,
16: 455-472., articleTitle=Structure-activity relationships of neuroactive steroids acting on the GABAA receptor, refAbstract=null), Reference(id=1220655539017662467, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.5b00032, pmid=null, pmcid=null, year=2015, volume=58, issue=null, pageStart=3500, pageEnd=3511, url=null, language=null, rfNumber=[23], rfOrder=22, authorNames=Botella GM, Salituro FG, Harrison BL, journalName=J Med Chem, refType=null, unstructuredReference=
Botella GM ,
Salituro FG ,
Harrison BL et al . Neuroactive steroids. 1. Positive allosteric modulators of the (
γ-aminobutyric acid)
A receptor:structure-activity relationships of heterocyclic substitution at C21[J].
J Med Chem,
2015,
58: 3500-3511., articleTitle=Neuroactive steroids. 1. Positive allosteric modulators of the (
γ-aminobutyric acid)
A receptor:structure-activity relationships of heterocyclic substitution at C21, refAbstract=null), Reference(id=1220655539139297294, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.7b00846, pmid=null, pmcid=null, year=2017, volume=60, issue=null, pageStart=7810, pageEnd=7819, url=null, language=null, rfNumber=[24], rfOrder=23, authorNames=Botella GM, Salituro FG, Harrison BL, journalName=J Med Chem, refType=null, unstructuredReference=
Botella GM ,
Salituro FG ,
Harrison BL et al . Neuroactive steroids. 2. 3
α-Hydroxy-3
β-methyl-21-(4-cyano-1
H-pyrazol-1'-yl)-19-nor-5
β-pregnan-20-one (SAGE-217):a clinical next generation neuroactive steroid positive allosteric modulator of the (
γ-aminobutyric acid)
A receptor[J].
J Med Chem,
2017,
60: 7810-7819., articleTitle=Neuroactive steroids. 2. 3
α-Hydroxy-3
β-methyl-21-(4-cyano-1
H-pyrazol-1'-yl)-19-nor-5
β-pregnan-20-one (SAGE-217):a clinical next generation neuroactive steroid positive allosteric modulator of the (
γ-aminobutyric acid)
A receptor, refAbstract=null), Reference(id=1220655539248349207, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm500695e, pmid=null, pmcid=null, year=2015, volume=58, issue=null, pageStart=525, pageEnd=536, url=null, language=null, rfNumber=[25], rfOrder=24, authorNames=Bourbeau MP, Bartberger MD, journalName=J Med Chem, refType=null, unstructuredReference=
Bourbeau MP ,
Bartberger MD . Recent advances in the development of acetyl-CoA carboxylase (ACC) inhibitors for the treatment of metabolic disease[J].
J Med Chem,
2015,
58: 525-536., articleTitle=Recent advances in the development of acetyl-CoA carboxylase (ACC) inhibitors for the treatment of metabolic disease, refAbstract=null), Reference(id=1220655539374178341, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1073/pnas.1509494113, pmid=null, pmcid=null, year=2016, volume=113, issue=null, pageStart=1796, pageEnd=1805, url=null, language=null, rfNumber=[26], rfOrder=25, authorNames=Harriman G, Greenwood J, Bhat S, journalName=Proc Natl Acad Sci U S A, refType=null, unstructuredReference=
Harriman G ,
Greenwood J ,
Bhat S et al . Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats[J].
Proc Natl Acad Sci U S A,
2016,
113: 1796-1805., articleTitle=Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats, refAbstract=null), Reference(id=1220655539546144825, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm2007613, pmid=null, pmcid=null, year=2011, volume=54, issue=null, pageStart=6342, pageEnd=6363, url=null, language=null, rfNumber=[27], rfOrder=26, authorNames=Cui JJ, Tran-Dubé M, Shen H, journalName=J Med Chem, refType=null, unstructuredReference=
Cui JJ ,
Tran-Dubé M ,
Shen H et al . Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK)[J].
J Med Chem,
2011,
54: 6342-6363., articleTitle=Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK), refAbstract=null), Reference(id=1220655539646808135, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm500261q, pmid=null, pmcid=null, year=2014, volume=57, issue=null, pageStart=4720, pageEnd=4744, url=null, language=null, rfNumber=[28], rfOrder=27, authorNames=Johnson TW, Richardson PF, Bailey S, journalName=J Med Chem, refType=null, unstructuredReference=
Johnson TW ,
Richardson PF ,
Bailey S et al . Discovery of (10
R)-7-amino-12-fluoro-2, 10, 16-trimethyl-15-oxo-10, 15, 16, 17-tetrahydro-2
H-8, 4-(metheno)pyrazolo[4, 3-h] [2, 5, 11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1(ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations[J].
J Med Chem,
2014,
57: 4720-4744., articleTitle=Discovery of (10
R)-7-amino-12-fluoro-2, 10, 16-trimethyl-15-oxo-10, 15, 16, 17-tetrahydro-2
H-8, 4-(metheno)pyrazolo[4, 3-h] [2, 5, 11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1(ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations, refAbstract=null), Reference(id=1220655539797803090, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=null, pmid=null, pmcid=null, year=2014, volume=49, issue=null, pageStart=1353, pageEnd=1356, url=null, language=null, rfNumber=[29], rfOrder=28, authorNames=Guo ZR, journalName=Acta Pharm Sin (药学学报), refType=null, unstructuredReference=
Guo ZR . From protein substrate to hepatitis C drug simeprevir[J].
Acta Pharm Sin (药学学报),
2014,
49: 1353-1356., articleTitle=From protein substrate to hepatitis C drug simeprevir, refAbstract=null), Reference(id=1220655539932020832, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.5b00788, pmid=null, pmcid=null, year=2015, volume=58, issue=null, pageStart=6225, pageEnd=6236, url=null, language=null, rfNumber=[30], rfOrder=29, authorNames=Priestley ES, Cheney DL, DeLucca I, journalName=J Med Chem, refType=null, unstructuredReference=
Priestley ES ,
Cheney DL ,
DeLucca I et al . Structure-based design of macrocyclic coagulation factor VⅡa inhibitors[J].
J Med Chem,
2015,
58: 6225-6236., articleTitle=Structure-based design of macrocyclic coagulation factor VⅡa inhibitors, refAbstract=null), Reference(id=1220655540028489834, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.6b01460, pmid=null, pmcid=null, year=2017, volume=60, issue=null, pageStart=1060, pageEnd=1067, url=null, language=null, rfNumber=[31], rfOrder=30, authorNames=Corte JR, Fang TA, Osuna H, journalName=J Med Chem, refType=null, unstructuredReference=
Corte JR ,
Fang TA ,
Osuna H et al . Structure-based design of macrocyclic factor XIa inhibitors:discovery of the macrocyclic amide linker[J].
J Med Chem,
2017,
60: 1060-1067., articleTitle=Structure-based design of macrocyclic factor XIa inhibitors:discovery of the macrocyclic amide linker, refAbstract=null), Reference(id=1220655540116570230, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1016/j.cbpa.2017.06.014, pmid=null, pmcid=null, year=2017, volume=39, issue=null, pageStart=133, pageEnd=142, url=null, language=null, rfNumber=[32], rfOrder=31, authorNames=Garner TP, Lopez A, Reyna DE, journalName=Curr Opin Chem Biol, refType=null, unstructuredReference=
Garner TP ,
Lopez A ,
Reyna DE et al . Progress in targeting the BCL-2 family of proteins[J].
Curr Opin Chem Biol,
2017,
39: 133-142., articleTitle=Progress in targeting the BCL-2 family of proteins, refAbstract=null), Reference(id=1220655540204650623, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm100863x, pmid=null, pmcid=null, year=2010, volume=53, issue=null, pageStart=7202, pageEnd=7218, url=null, language=null, rfNumber=[33], rfOrder=32, authorNames=Sofia MJ, Bao DH, Chang W, journalName=J Med Chem, refType=null, unstructuredReference=
Sofia MJ ,
Bao DH ,
Chang W et al . Discovery of a
β-
D-2'-deoxy-2'-
α-fluoro-2'-
β-
C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus[J].
J Med Chem,
2010,
53: 7202-7218., articleTitle=Discovery of a
β-
D-2'-deoxy-2'-
α-fluoro-2'-
β-
C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus, refAbstract=null), Reference(id=1220655540301119625, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.6b01594, pmid=null, pmcid=null, year=2017, volume=60, issue=null, pageStart=1648, pageEnd=1661, url=null, language=null, rfNumber=[34], rfOrder=33, authorNames=Siegel D, Hui HC, Doerffler E, journalName=J Med Chem, refType=null, unstructuredReference=
Siegel D ,
Hui HC ,
Doerffler E et al . Discovery and synthesis of a phosphoramidate prodrug of a pyrrolo[2, 1f] [triazin-4-amino] adenine
C-nucleoside (GS-5734) for the treatment of Ebola and emerging viruses[J].
J Med Chem,
2017,
60: 1648-1661., articleTitle=Discovery and synthesis of a phosphoramidate prodrug of a pyrrolo[2, 1f] [triazin-4-amino] adenine
C-nucleoside (GS-5734) for the treatment of Ebola and emerging viruses, refAbstract=null), Reference(id=1220655540401782937, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=null, pmid=null, pmcid=null, year=2013, volume=33, issue=null, pageStart=3879, pageEnd=3885, url=http://med.wanfangdata.com.cn/Paper/Detail/PeriodicalPaper_PM24023323, language=null, rfNumber=[35], rfOrder=34, authorNames=Cao H, Yamamoto K, Yang LX, journalName=Anticancer Res, refType=null, unstructuredReference=
Cao H ,
Yamamoto K ,
Yang LX et al . Brentuximab vedotin:first-line agent for advanced Hodgkin lymphoma[J].
Anticancer Res,
2013,
33: 3879-3885., articleTitle=Brentuximab vedotin:first-line agent for advanced Hodgkin lymphoma, refAbstract=null), Reference(id=1220655540523417765, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/ar700108g, pmid=null, pmcid=null, year=2008, volume=41, issue=null, pageStart=98, pageEnd=107, url=null, language=null, rfNumber=[36], rfOrder=35, authorNames=Chari RV, journalName=Acc Chem Res, refType=null, unstructuredReference=
Chari RV . Targeted cancer therapy:conferring specificity to cytotoxic drugs[J].
Acc Chem Res,
2008,
41: 98-107., articleTitle=Targeted cancer therapy:conferring specificity to cytotoxic drugs, refAbstract=null), Reference(id=1220655540632469677, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1177/0091270004267595, pmid=null, pmcid=null, year=2004, volume=44, issue=null, pageStart=873, pageEnd=880, url=null, language=null, rfNumber=[37], rfOrder=36, authorNames=Buckwalter M, Dowell JA, Korth-Bradley J, journalName=J Clin Pharmacol, refType=null, unstructuredReference=
Buckwalter M ,
Dowell JA ,
Korth-Bradley J et al . Pharmacokinetics of gemtuzumab ozogamicin as a single-agent treatment of pediatric patients with refractory or relapsed acute myeloid leukemia[J].
J Clin Pharmacol,
2004,
44: 873-880., articleTitle=Pharmacokinetics of gemtuzumab ozogamicin as a single-agent treatment of pediatric patients with refractory or relapsed acute myeloid leukemia, refAbstract=null), Reference(id=1220655540770881722, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1056/NEJMoa1914510, pmid=null, pmcid=null, year=2020, volume=382, issue=null, pageStart=610, pageEnd=621, url=null, language=null, rfNumber=[38], rfOrder=37, authorNames=Modi S, Saura C, Yamashita T, journalName=New Engl J Med, refType=null, unstructuredReference=
Modi S ,
Saura C ,
Yamashita T et al . Trastuzumab deruxtecan in previously treated HER2-positive breast cancer[J].
New Engl J Med,
2020,
382: 610-621., articleTitle=Trastuzumab deruxtecan in previously treated HER2-positive breast cancer, refAbstract=null), Reference(id=1220655540854767810, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1158/0008-5472.CAN-07-0033, pmid=null, pmcid=null, year=2007, volume=67, issue=null, pageStart=4434, pageEnd=4442, url=null, language=null, rfNumber=[39], rfOrder=38, authorNames=Reddy JA, Dorton R, Westrick E, journalName=Cancer Res, refType=null, unstructuredReference=
Reddy JA ,
Dorton R ,
Westrick E et al . Preclinical evaluation of EC145, a folate-vinca alkaloid conjugate[J].
Cancer Res,
2007,
67: 4434-4442., articleTitle=Preclinical evaluation of EC145, a folate-vinca alkaloid conjugate, refAbstract=null), Reference(id=1220655540934459590, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1016/j.ab.2004.12.026, pmid=null, pmcid=null, year=2005, volume=338, issue=null, pageStart=284, pageEnd=293, url=null, language=null, rfNumber=[40], rfOrder=39, authorNames=Parker N, Turk MJ, Westrick E, journalName=Anal Biochem, refType=null, unstructuredReference=
Parker N ,
Turk MJ ,
Westrick E et al . Folate receptor expression in carcinomas and normal tissues determined by a quantitative radioligand binding assay[J].
Anal Biochem,
2005,
338: 284-293., articleTitle=Folate receptor expression in carcinomas and normal tissues determined by a quantitative radioligand binding assay, refAbstract=null), Reference(id=1220655541022539983, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.8b02036, pmid=null, pmcid=null, year=2019, volume=62, issue=null, pageStart=2708, pageEnd=2719, url=null, language=null, rfNumber=[41], rfOrder=40, authorNames=White BH, Whalen K, Kriksciukaite K, journalName=J Med Chem, refType=null, unstructuredReference=
White BH ,
Whalen K ,
Kriksciukaite K et al . Discovery of an SSTR2-targeting maytansinoid conjugate (PEN-221) with potent activity
in vitro and
in vivo[J].
J Med Chem,
2019,
62: 2708-2719., articleTitle=Discovery of an SSTR2-targeting maytansinoid conjugate (PEN-221) with potent activity
in vitro and
in vivo, refAbstract=null), Reference(id=1220655541102231769, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=null, pmid=null, pmcid=null, year=2018, volume=62, issue=null, pageStart=1, pageEnd=11, url=null, language=null, rfNumber=[42], rfOrder=41, authorNames=Ito A, Sato T, Ota M, journalName=Antimicrob Agents Chemother, refType=null, unstructuredReference=
Ito A ,
Sato T ,
Ota M et al .
In vitro antibacterial properties of cefiderocol, a novel siderophore cephalosporin, against gram-negative bacteria[J].
Antimicrob Agents Chemother,
2018,
62: 1-11., articleTitle=
In vitro antibacterial properties of cefiderocol, a novel siderophore cephalosporin, against gram-negative bacteria, refAbstract=null), Reference(id=1220655541181923551, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=null, pmid=null, pmcid=null, year=2016, volume=9, issue=null, pageStart=8, pageEnd=18, url=null, language=null, rfNumber=[43], rfOrder=42, authorNames=Breeman WA, Chan HS, de Zanger RM, journalName=Curr Radiopharm, refType=null, unstructuredReference=
Breeman WA ,
Chan HS ,
de Zanger RM et al . Overview of development and formulation of
177Lu-DOTATATE for PRRT[J].
Curr Radiopharm,
2016,
9: 8-18., articleTitle=Overview of development and formulation of
177Lu-DOTATATE for PRRT, refAbstract=null), Reference(id=1220655541299364071, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1038/nsmb.2874, pmid=null, pmcid=null, year=2014, volume=21, issue=null, pageStart=803, pageEnd=809, url=null, language=null, rfNumber=[44], rfOrder=43, authorNames=Chamberlain PP, Lopez-Girona A, Miller K, journalName=Nat Struct Mol Biol, refType=null, unstructuredReference=
Chamberlain PP ,
Lopez-Girona A ,
Miller K et al . Structure of the human cereblon-DDB1-lenalidomide complex reveals basis for responsiveness to thalidomide analogs[J].
Nat Struct Mol Biol,
2014,
21: 803-809., articleTitle=Structure of the human cereblon-DDB1-lenalidomide complex reveals basis for responsiveness to thalidomide analogs, refAbstract=null), Reference(id=1220655541404221679, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm5011258, pmid=null, pmcid=null, year=2014, volume=57, issue=null, pageStart=8657, pageEnd=8663, url=null, language=null, rfNumber=[45], rfOrder=44, authorNames=Galdeano C, Gadd MS, Soares P, journalName=J Med Chem, refType=null, unstructuredReference=
Galdeano C ,
Gadd MS ,
Soares P et al . Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with
in vitro nanomolar affinities[J].
J Med Chem,
2014,
57: 8657-8663., articleTitle=Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with
in vitro nanomolar affinities, refAbstract=null), Reference(id=1220655541534245111, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1126/science.1092472, pmid=null, pmcid=null, year=2004, volume=303, issue=null, pageStart=844, pageEnd=848, url=null, language=null, rfNumber=[46], rfOrder=45, authorNames=Vassilev LT, Vu BT, Graves B, journalName=Science, refType=null, unstructuredReference=
Vassilev LT ,
Vu BT ,
Graves B et al .
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2[J].
Science,
2004,
303: 844-848., articleTitle=
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2, refAbstract=null), Reference(id=1220655541664268543, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1016/j.bmcl.2008.07.114, pmid=null, pmcid=null, year=2008, volume=18, issue=null, pageStart=5904, pageEnd=5908, url=null, language=null, rfNumber=[47], rfOrder=46, authorNames=Schneekloth AR, Pucheault M, Tae HS, journalName=Bioorg Med Chem Lett, refType=null, unstructuredReference=
Schneekloth AR ,
Pucheault M ,
Tae HS et al . Targeted intracellular protein degradation induced by a small molecule:En route to chemical proteomics[J].
Bioorg Med Chem Lett,
2008,
18: 5904-5908., articleTitle=Targeted intracellular protein degradation induced by a small molecule:En route to chemical proteomics, refAbstract=null), Reference(id=1220655541983035656, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/ja100691p, pmid=null, pmcid=null, year=2010, volume=132, issue=null, pageStart=5820, pageEnd=5826, url=null, language=null, rfNumber=[48], rfOrder=47, authorNames=Itoh Y, Ishikawa M, Naito M, journalName=J Am Chem Soc, refType=null, unstructuredReference=
Itoh Y ,
Ishikawa M ,
Naito M et al . Protein knockdown using methyl bestatin-ligand hybrid molecules:design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins[J].
J Am Chem Soc,
2010,
132: 5820-5826., articleTitle=Protein knockdown using methyl bestatin-ligand hybrid molecules:design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins, refAbstract=null), Reference(id=1220655542087893260, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1080/17460441.2019.1659242, pmid=null, pmcid=null, year=2019, volume=14, issue=null, pageStart=1255, pageEnd=1268, url=null, language=null, rfNumber=[49], rfOrder=48, authorNames=Konstantinidou M, Li JY, Zhang BD, journalName=Expert Opin Drug Discov, refType=null, unstructuredReference=
Konstantinidou M ,
Li JY ,
Zhang BD et al . PROTACs-a game-changing technology[J].
Expert Opin Drug Discov,
2019,
14: 1255-1268., articleTitle=PROTACs-a game-changing technology, refAbstract=null), Reference(id=1220655542175973651, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.8b01631, pmid=null, pmcid=null, year=2019, volume=62, issue=null, pageStart=941, pageEnd=964, url=null, language=null, rfNumber=[50], rfOrder=49, authorNames=Han X, Wang C, Qin C, journalName=J Med Chem, refType=null, unstructuredReference=
Han X ,
Wang C ,
Qin C et al . Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer[J].
J Med Chem,
2019,
62: 941-964., articleTitle=Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer, refAbstract=null), Reference(id=1220655542268248348, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.9b01393, pmid=null, pmcid=null, year=2019, volume=62, issue=null, pageStart=11218, pageEnd=11231, url=null, language=null, rfNumber=[51], rfOrder=50, authorNames=Han X, Zhao LJ, Xiang WG, journalName=J Med Chem, refType=null, unstructuredReference=
Han X ,
Zhao LJ ,
Xiang WG et al . Discovery of highly potent and efficient PROTAC degraders of androgen receptor (AR) by employing weak binding affinity VHL E3 ligase ligands[J].
J Med Chem,
2019,
62: 11218-11231., articleTitle=Discovery of highly potent and efficient PROTAC degraders of androgen receptor (AR) by employing weak binding affinity VHL E3 ligase ligands, refAbstract=null), Reference(id=1220655542368911656, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1038/s41422-018-0055-1, pmid=null, pmcid=null, year=2018, volume=28, issue=null, pageStart=779, pageEnd=781, url=null, language=null, rfNumber=[52], rfOrder=51, authorNames=Sun YH, Zhao XW, Ding N, journalName=Cell Res, refType=null, unstructuredReference=
Sun YH ,
Zhao XW ,
Ding N et al . PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies[J].
Cell Res,
2018,
28: 779-781., articleTitle=PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies, refAbstract=null), Reference(id=1220655542469574963, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1016/j.chembiol.2015.05.009, pmid=null, pmcid=null, year=2015, volume=22, issue=null, pageStart=755, pageEnd=763, url=null, language=null, rfNumber=[53], rfOrder=52, authorNames=Lu J, Qian Y, Altieri M, journalName=Chem Biol, refType=null, unstructuredReference=
Lu J ,
Qian Y ,
Altieri M et al . Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4[J].
Chem Biol,
2015,
22: 755-763., articleTitle=Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4, refAbstract=null), Reference(id=1220655542616375612, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.8b01572, pmid=null, pmcid=null, year=2019, volume=62, issue=null, pageStart=1420, pageEnd=1442, url=null, language=null, rfNumber=[54], rfOrder=53, authorNames=Hu J, Hu B, Wang M, journalName=J Med Chem, refType=null, unstructuredReference=
Hu J ,
Hu B ,
Wang M et al . Discovery of ERD-308 as a highly potent proteolysis targeting chimera (PROTAC) degrader of estrogen receptor (ER)[J].
J Med Chem,
2019,
62: 1420-1442., articleTitle=Discovery of ERD-308 as a highly potent proteolysis targeting chimera (PROTAC) degrader of estrogen receptor (ER), refAbstract=null), Reference(id=1220655542738010442, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/acs.jmedchem.9b01566, pmid=null, pmcid=null, year=2020, volume=63, issue=null, pageStart=1216, pageEnd=1232, url=null, language=null, rfNumber=[55], rfOrder=54, authorNames=Cheng M, Yu XF, Lu K, journalName=J Med Chem, refType=null, unstructuredReference=
Cheng M ,
Yu XF ,
Lu K et al . Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders[J].
J Med Chem,
2020,
63: 1216-1232., articleTitle=Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders, refAbstract=null), Reference(id=1220655542830285138, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, doi=10.1021/jm800669s, pmid=null, pmcid=null, year=2008, volume=51, issue=null, pageStart=6902, pageEnd=6915, url=null, language=null, rfNumber=[56], rfOrder=55, authorNames=Park CM, Bruncko M, Adickes J, journalName=J Med Chem, refType=null, unstructuredReference=
Park CM ,
Bruncko M ,
Adickes J et al . Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins[J].
J Med Chem,
2008,
51: 6902-6915., articleTitle=Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins, refAbstract=null)], funds=null, companyList=[AuthorCompany(id=1220655530754884082, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, xref=null, ext=[AuthorCompanyExt(id=1220655530763272691, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, companyId=1220655530754884082, language=EN, country=null, province=null, city=null, postcode=null, companyName=null, departmentName=null, remark=Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China), AuthorCompanyExt(id=1220655530771661301, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, companyId=1220655530754884082, language=CN, country=null, province=null, city=null, postcode=null, companyName=null, departmentName=null, remark=中国医学科学院、北京协和医学院药物研究所, 北京 100050)])], figs=[ArticleFig(id=1220655532440994388, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=a58/SlPFaiPsWlKOlEtHmg==, figureFileBig=ExFEmXxp7FgrlBrKqyHUOQ==, tableContent=null), ArticleFig(id=1220655532516491865, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 1, caption=
The comparison of binding mode between ibrutinib (8) and zanubrutinib (10) , figureFileSmall=a58/SlPFaiPsWlKOlEtHmg==, figureFileBig=ExFEmXxp7FgrlBrKqyHUOQ==, tableContent=null), ArticleFig(id=1220655532722012771, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=SJvz5MwOzxvXdlo8OAL/Qg==, figureFileBig=IDCI/DudCHdg477lYkvyHQ==, tableContent=null), ArticleFig(id=1220655532822676074, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 2, caption=
Binding mode of crystallography for baceprevir-NS3 complex , figureFileSmall=SJvz5MwOzxvXdlo8OAL/Qg==, figureFileBig=IDCI/DudCHdg477lYkvyHQ==, tableContent=null), ArticleFig(id=1220655532931727983, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=icI0xvGvQjpDJqZy2C6GQg==, figureFileBig=KHUDSl3eZGABiFkKjOXmBw==, tableContent=null), ArticleFig(id=1220655533049168503, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 3, caption=
a. Sketch map of imatinib binding to critical residues of wild Abl; b. Docking diagram of ponatinib to AblT315I , figureFileSmall=icI0xvGvQjpDJqZy2C6GQg==, figureFileBig=KHUDSl3eZGABiFkKjOXmBw==, tableContent=null), ArticleFig(id=1220655533154026111, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=YM2JJPreQJsuZFoaIVJQTA==, figureFileBig=JiR/3KdLFZ3+vMRdog2BHQ==, tableContent=null), ArticleFig(id=1220655533242106499, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 4, caption=
Binding diagram of AMG-510 (22) to GDP-KRASG12C , figureFileSmall=YM2JJPreQJsuZFoaIVJQTA==, figureFileBig=JiR/3KdLFZ3+vMRdog2BHQ==, tableContent=null), ArticleFig(id=1220655533346964106, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=gbwR7Gj5zlOBQtAD3MWFxw==, figureFileBig=0cEKfdBftDs86GeS9GslHg==, tableContent=null), ArticleFig(id=1220655533439238796, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 5, caption=
Asciminib binds to allosteric domain, different from nilotinib which binds to ATP binding site , figureFileSmall=gbwR7Gj5zlOBQtAD3MWFxw==, figureFileBig=0cEKfdBftDs86GeS9GslHg==, tableContent=null), ArticleFig(id=1220655533556679313, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=SzaukNsQzYmPhood45Fndw==, figureFileBig=BwhZ2eqU6CieqFWYZc8+FQ==, tableContent=null), ArticleFig(id=1220655533661536919, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 6, caption=
Schematic depicting various ACC domains and their functions , figureFileSmall=SzaukNsQzYmPhood45Fndw==, figureFileBig=BwhZ2eqU6CieqFWYZc8+FQ==, tableContent=null), ArticleFig(id=1220655533778977439, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=Uu0jLf9LGg9r6Ue8bypSoQ==, figureFileBig=ZqPqIqkMClAPSkdbqGsnEA==, tableContent=null), ArticleFig(id=1220655533871252130, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 7, caption=
a. Cocrystal structure of 27 complexed with hACC2 BC overlaid with the structure of hACC2 BC complexed with soraphen A(26). b. Structure of firsocostat (28) modeled into the cocrystal structure of its amide complexed with hACC2 BC , figureFileSmall=Uu0jLf9LGg9r6Ue8bypSoQ==, figureFileBig=ZqPqIqkMClAPSkdbqGsnEA==, tableContent=null), ArticleFig(id=1220655533988692651, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=tJtYHaokEF6oVaHchBwswQ==, figureFileBig=AVNtU7F24WDYkl00v7bG1w==, tableContent=null), ArticleFig(id=1220655534110327469, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 8, caption=
Crystallography of ALK-crizotinib complex and the mutation sites of ALK , figureFileSmall=tJtYHaokEF6oVaHchBwswQ==, figureFileBig=AVNtU7F24WDYkl00v7bG1w==, tableContent=null), ArticleFig(id=1220655534231962295, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=wQ95pwYDKMC9jEN7PSb7vQ==, figureFileBig=/tr/3j0rLZqwEabjMJBFbw==, tableContent=null), ArticleFig(id=1220655534315848379, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 9, caption=
Evolutional scheme of crizotinib (29) to macromolecule lorlatinib (30) via typical compounds , figureFileSmall=wQ95pwYDKMC9jEN7PSb7vQ==, figureFileBig=/tr/3j0rLZqwEabjMJBFbw==, tableContent=null), ArticleFig(id=1220655534399734466, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=qXq1zvzpLjZIlgB6Sw/i3Q==, figureFileBig=GHeTB/7O7tznDYehxwfTvg==, tableContent=null), ArticleFig(id=1220655534479426245, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 10, caption=
Crystal structure of 37 bound to FVIIa. The proximity of the P1′ acetanilide and P2 phenyl groups suggested that macrocyclization was feasible, as indicated by the double-headed yellow arrow , figureFileSmall=qXq1zvzpLjZIlgB6Sw/i3Q==, figureFileBig=GHeTB/7O7tznDYehxwfTvg==, tableContent=null), ArticleFig(id=1220655534580089543, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=k18Tc1Oytr9ohqiDXrFahg==, figureFileBig=ZcILjrdo8a/thE02O4FVWQ==, tableContent=null), ArticleFig(id=1220655534655587022, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 11, caption=
a. General structure for optimization of macrocycle size; b. Crystallographic structure of (R)-38 in FVIIa; c. Overlay of 37 (white) and (R)-38 (yellow) bound to FVIIa , figureFileSmall=k18Tc1Oytr9ohqiDXrFahg==, figureFileBig=ZcILjrdo8a/thE02O4FVWQ==, tableContent=null), ArticleFig(id=1220655534739473107, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=bMSzGZdwkdnCDcLFf96g9g==, figureFileBig=hMFHP+Kyy13fvatAjrxBFg==, tableContent=null), ArticleFig(id=1220655534819164890, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 12, caption=
X-ray crystal structure of acyclic phenyl imidazole 40 in factor XIa , figureFileSmall=bMSzGZdwkdnCDcLFf96g9g==, figureFileBig=hMFHP+Kyy13fvatAjrxBFg==, tableContent=null), ArticleFig(id=1220655535125349087, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=WXRhr2ZEDh5cGx1JJ/NZpw==, figureFileBig=uQ3GIBYBFlD1mtXb7d4SCw==, tableContent=null), ArticleFig(id=1220655535276344041, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 13, caption=
X-ray crystal structure of 42 bound to factor XIa , figureFileSmall=WXRhr2ZEDh5cGx1JJ/NZpw==, figureFileBig=uQ3GIBYBFlD1mtXb7d4SCw==, tableContent=null), ArticleFig(id=1220655535372813038, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=7wbb3pk0s1v76XwJ4VmJDA==, figureFileBig=y/GYSnjCsdEaRh0cPjK2fg==, tableContent=null), ArticleFig(id=1220655535460893428, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 14, caption=
Sketch of the binding mode of imatinib to Abl , figureFileSmall=7wbb3pk0s1v76XwJ4VmJDA==, figureFileBig=y/GYSnjCsdEaRh0cPjK2fg==, tableContent=null), ArticleFig(id=1220655535561556730, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=xbb7siBI71JU6f27Zc9wkw==, figureFileBig=t+Bf+8jWvQLhvBXKgXcRFw==, tableContent=null), ArticleFig(id=1220655535662220032, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 15, caption=
Sketch of the process in ADC action , figureFileSmall=xbb7siBI71JU6f27Zc9wkw==, figureFileBig=t+Bf+8jWvQLhvBXKgXcRFw==, tableContent=null), ArticleFig(id=1220655535771271945, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=z3QSrRl/zZV1HnMP9UbMKw==, figureFileBig=6H2R19vGwFm0qHVDWRV3JA==, tableContent=null), ArticleFig(id=1220655535871935247, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 16, caption=
Sketch of event-driven pharmacology of PROTAC molecule , figureFileSmall=z3QSrRl/zZV1HnMP9UbMKw==, figureFileBig=6H2R19vGwFm0qHVDWRV3JA==, tableContent=null), ArticleFig(id=1220655535989375763, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=WtmVSniGzY4qhRx4grNamw==, figureFileBig=FPT1E60RZ6gLOAAQIjtCAA==, tableContent=null), ArticleFig(id=1220655536102621981, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Figure 17, caption=
Typical structures of E3 ligase recruiter , figureFileSmall=WtmVSniGzY4qhRx4grNamw==, figureFileBig=FPT1E60RZ6gLOAAQIjtCAA==, tableContent=null), ArticleFig(id=1220655536228451110, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=EN, label=null, caption=null, figureFileSmall=null, figureFileBig=null, tableContent=
| Generic name | Trade name | Composition | Target | Indication | Lounch time/company |
| Brentuximab vedotin | Adcetris | Brentuximab/vedotin | CD30 | Hodgkin's lymphoma, ALCL | 2011-08 Seattle/Takeda |
| Trastuzumab emtansine | Kadcyla | Trastuzumab/maitansine | HER2 | Breast cancer | 2013-02 Genetech/Roche |
| Gemturumab ozogamicin | Mylotarg | Gemturumab/ozogamicin | CD33 | AML | 2017-01 Wyeth/Pfizer |
| Inoturumab ozogamicin | Besponsa | Inoturumab/ozogamicin | CD22 | Lymphocytic leukemia | 2017-08 Wyeth/Pfizer |
| Polaturumab vedotin | Polivy | Polaturumab/vedotin | CD79 | Large B-cell lymphoma | |
| Enfortumab vedotin | Padcev | Enfortumab/vedotin | Nectin-4 | Urothelial carcinoma | 2019-12 Seattle/Astellas |
| fam-Trastuzumab deruxatecan-nxki | Enhertu | Trastuzumab/deruxatecan | HER2 | Breast cancer | 2019-12 Daiichi-Sankyo/AstraZeneca |
), ArticleFig(id=1220655536358474543, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1220655524194992260, language=CN, label=Table 1, caption=
List of ADC approved by FDA. ALCL: Anaplastic large cell lymphoma; AML: Acute myeloid leukemia
, figureFileSmall=null, figureFileBig=null, tableContent=
| Generic name | Trade name | Composition | Target | Indication | Lounch time/company |
| Brentuximab vedotin | Adcetris | Brentuximab/vedotin | CD30 | Hodgkin's lymphoma, ALCL | 2011-08 Seattle/Takeda |
| Trastuzumab emtansine | Kadcyla | Trastuzumab/maitansine | HER2 | Breast cancer | 2013-02 Genetech/Roche |
| Gemturumab ozogamicin | Mylotarg | Gemturumab/ozogamicin | CD33 | AML | 2017-01 Wyeth/Pfizer |
| Inoturumab ozogamicin | Besponsa | Inoturumab/ozogamicin | CD22 | Lymphocytic leukemia | 2017-08 Wyeth/Pfizer |
| Polaturumab vedotin | Polivy | Polaturumab/vedotin | CD79 | Large B-cell lymphoma | |
| Enfortumab vedotin | Padcev | Enfortumab/vedotin | Nectin-4 | Urothelial carcinoma | 2019-12 Seattle/Astellas |
| fam-Trastuzumab deruxatecan-nxki | Enhertu | Trastuzumab/deruxatecan | HER2 | Breast cancer | 2019-12 Daiichi-Sankyo/AstraZeneca |
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