Article(id=1208489285485970143, tenantId=1146029695717560320, journalId=1189982191388893191, issueId=1208489268704555590, articleNumber=null, orderNo=null, doi=10.16438/j.0513-4870.2021-1108, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=research-article, receivedDate=1627315200000, receivedDateStr=2021-07-27, revisedDate=1628697600000, revisedDateStr=2021-08-12, acceptedDate=null, acceptedDateStr=null, onlineDate=1766055898305, onlineDateStr=2025-12-18, pubDate=1633968000000, pubDateStr=2021-10-12, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1766055898305, onlineIssueDateStr=2025-12-18, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1766055898305, creator=13701087609, updateTime=1766055898305, updator=13701087609, issue=Issue{id=1208489268704555590, tenantId=1146029695717560320, journalId=1189982191388893191, year='2021', volume='56', issue='10', pageStart='2597', pageEnd='2880', issueExtLink='null', onlineDate='null', pubDate='null', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1766055894304, creator=13701087609, updateTime=1766137041718, updator=13701087609, preIssue=null, nextIssue=null, ext={EN=IssueExt(id=1208829625678033640, tenantId=1146029695717560320, journalId=1189982191388893191, issueId=1208489268704555590, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1208829625682227945, tenantId=1146029695717560320, journalId=1189982191388893191, issueId=1208489268704555590, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null}, startPage=2682, endPage=2688, ext={EN=ArticleExt(id=1208489287474070350, articleId=1208489285485970143, tenantId=1146029695717560320, journalId=1189982191388893191, language=EN, title=Molecular glue in drugs, columnId=1190335349059588909, journalTitle=Acta Pharmaceutica Sinica, columnName=Professionals Forum, runingTitle=null, highlight=null, articleAbstract=
Most small molecule drugs bind to enzymes, receptors or ion channels, which possess binding pocket for drug occupation. However, the study of drugs that interfere with protein-protein interactions has always been a challenging subject. The discovery of molecular glues and degraders has opened an avenue to tackle this issue. With the structural features of bifunctional ligand molecular glues mediate the recognition and binding of two proteins. As a useful tool for chemical biology molecular glue can not only help to find probes to undruggable targets, but also can be developed into drugs through structure optimization in medicinal chemistry. This minireview concisely describes the features of molecular glue using a few existing drugs or active compounds.
, correspAuthors=Zong-ru GUO, authorNote=null, correspAuthorsNote=null, copyrightStatement=Copyright ©2021 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=1208489291932614822, articleId=1208489285485970143, tenantId=1146029695717560320, journalId=1189982191388893191, language=CN, title=药物中的分子胶, columnId=1190335349206389552, journalTitle=药学学报, columnName=专家论坛, runingTitle=null, highlight=null, articleAbstract=
大多数药物的作用靶标是蛋白质，研究干预蛋白-蛋白相互作用的药物向来是具有挑战性的课题，分子胶和分子胶降解剂的发现开辟了新的途径。分子胶在结构上具有双功能的配体特征，介导两个蛋白的识别与结合，既可成为发现非可药性靶标的切入点，是化学生物学的有用工具，也可经药物化学的优化发展成为药物。本文以现有的分子胶药物或活性化合物为例简要叙述分子胶的特征。
, correspAuthors=郭宗儒, authorNote=null, correspAuthorsNote=
, copyrightStatement=版权所有©《药学学报》编辑部2021, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=PZSN6vGqNVJqdpcWxNwJsQ==, magXml=Qvxb90ATHwTSvh2LbLyshw==, pdfUrl=null, pdf=nrVfAZlAI9drXW1YCB6fNA==, pdfFileSize=717858, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=FMOfTByWxNcwGsxmjeEuew==, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=lM9+DdmDGq1afhQgBqwgAw==, mapNumber=null, authorCompany=null, fund=null, authors=null, authorsList=郭宗儒)}, authors=[Author(id=1208489292536594647, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, 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=1208489292796641507, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, authorId=1208489292536594647, 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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*, address=中国医学科学院、北京协和医学院药物研究所, 北京 100050, bio=null, bioImg=null, bioContent=null, aboutCorrespAuthor=null)}, companyList=[AuthorCompany(id=1208489292389793991, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, xref=null, ext=[AuthorCompanyExt(id=1208489292398182599, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, companyId=1208489292389793991, 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=1208489292402376904, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, companyId=1208489292389793991, 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)])])], keywords=[Keyword(id=1208489293186711809, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, orderNo=1, keyword=molecular glue), Keyword(id=1208489293320929548, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, orderNo=2, keyword=degrader), Keyword(id=1208489293501284632, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, orderNo=3, keyword=cyclosporine A), Keyword(id=1208489293736165681, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, orderNo=4, keyword=lenalidomide), Keyword(id=1208489293857800506, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, orderNo=5, keyword=indisulam), Keyword(id=1208489293958463816, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, orderNo=6, keyword=polykitide), Keyword(id=1208489294050738514, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, orderNo=1, keyword=分子胶), Keyword(id=1208489294184956258, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, orderNo=2, keyword=降解剂), Keyword(id=1208489294294008171, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, orderNo=3, keyword=环孢菌素A), Keyword(id=1208489295535522173, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, orderNo=4, keyword=来那度胺), Keyword(id=1208489295673934220, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, orderNo=5, keyword=吲地苏兰), Keyword(id=1208489295795569049, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, orderNo=6, keyword=聚酮)], refs=[Reference(id=1208489297569759852, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, doi=10.1016/0092-8674(91)90124-H, pmid=null, pmcid=null, year=1991, volume=66, issue=null, pageStart=807, pageEnd=815, url=null, language=null, rfNumber=[1], rfOrder=0, authorNames=Liu J, Farmer JD, Lane WS, journalName=Cell, refType=null, unstructuredReference=
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The binding mode of the ternary complexes of cyclosporine A, tacrolimus, and rapamycin with the respective receptor and target protein<sup>[<a href="javascript:;" class="mag_content_a" onclick="piaofuRef(this,'b2')" rid="b2">2</a>]</sup> , figureFileSmall=qImQb4ompbr2682dIecO/A==, figureFileBig=FMOfTByWxNcwGsxmjeEuew==, tableContent=null), ArticleFig(id=1208489296546349551, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, label=null, caption=null, figureFileSmall=J8husAbi8J8Hh0E+gsylCQ==, figureFileBig=ZsNOj8HDj2PMZR0D4inGWg==, tableContent=null), ArticleFig(id=1208489296663790073, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, label=Figure 2, caption=
a: CRBN surface contacted by CK1<i>α</i> and IKZF1. b: CRBN binds the glutarimide moiety in a hydrophobic pocket. The phthalimide ring of lenalidomide is surface exposed. A <i>β</i>-hairpin loop of CK1<i>α</i> binds CRBN on top of its lenalidomide-binding pocket. c: Side-chain interactions between CK1<i>α</i>, CRBN and lenalidomide. Lenalidomide provides van der Waals interactions with CK1<i>α</i>. CRBN residues that form the hydrophobic pocket are shown in grey. Dashed lines indicate hydrogen bonds<sup>[<a href="javascript:;" class="mag_content_a" onclick="piaofuRef(this,'b7')" rid="b7">7</a>]</sup> , figureFileSmall=J8husAbi8J8Hh0E+gsylCQ==, figureFileBig=ZsNOj8HDj2PMZR0D4inGWg==, tableContent=null), ArticleFig(id=1208489296814785037, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, label=null, caption=null, figureFileSmall=Xe7pz8M4eIc4R7TmxQSenw==, figureFileBig=M6e99ruraxoW8X1NYfF2LQ==, tableContent=null), ArticleFig(id=1208489296915448341, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, label=Figure 3, caption=
Indisulam targets the splicing factor RBM39 for proteasomal degradation<sup>[<a href="javascript:;" class="mag_content_a" onclick="piaofuRef(this,'b8')" rid="b8">8</a>]</sup> , figureFileSmall=Xe7pz8M4eIc4R7TmxQSenw==, figureFileBig=M6e99ruraxoW8X1NYfF2LQ==, tableContent=null), ArticleFig(id=1208489297032888870, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, label=null, caption=null, figureFileSmall=X6iWjiz6Nrhz20geHWHpWQ==, figureFileBig=29d1uYiR6k5lTzoHfjJ5aw==, tableContent=null), ArticleFig(id=1208489297154523702, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, label=Figure 4, caption=
Indisulam-mediated interactions between DCAF15 and RBM39. Indisulam (orange) bridges the structure of DCAF15 (green) and RBM39 (magenta) by forming several direct or water-mediated interactions with both DCAF15 and RBM39 and serves to increase the complementarity between the two surfaces. Hydrogen bonds are shown as dotted lines and the surfaces of both DCAF15 and RBM39 are shown. Key residues are labeled<sup>[<a href="javascript:;" class="mag_content_a" onclick="piaofuRef(this,'b9')" rid="b9">9</a>]</sup> , figureFileSmall=X6iWjiz6Nrhz20geHWHpWQ==, figureFileBig=29d1uYiR6k5lTzoHfjJ5aw==, tableContent=null), ArticleFig(id=1208489297271964228, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=EN, label=null, caption=null, figureFileSmall=TBgd+y5GjRyJY9yoBgzq+Q==, figureFileBig=g97J7z7KeE85J6EwQAl5NA==, tableContent=null), ArticleFig(id=1208489297410376276, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1208489285485970143, language=CN, label=Figure 5, caption=
a: Cartoon representation of the crystal structure of DDB1 (∆BPB)-(R)-CR8-CDK12-cyclin K; b: Close-up view of the DDB1-CR8-CDK12 interface. The phenylpyridine moiety of CR8 contacts DDB1 residues<sup>[<a href="javascript:;" class="mag_content_a" onclick="piaofuRef(this,'b10')" rid="b10">10</a>]</sup> , figureFileSmall=TBgd+y5GjRyJY9yoBgzq+Q==, figureFileBig=g97J7z7KeE85J6EwQAl5NA==, tableContent=null)], attaches=null, journal=Journal(id=1189982048455397383, delFlag=0, nameCn=药学学报, nameEn=Acta Pharmaceutica Sinica, nameHistory1=null, nameHistory2=null, issn=0513-4870, eissn=null, cn=11-2163/R, coden=null, periodic=0, language=CN, oaType=null, ccby=null, superviseOffice=null, ownerOffice=null, pubOffice=null, editorOffice=null, officeType=null, aims=null, clcCode=null, officeProv=null, officeCity=null, officeAddr=null, officeZip=null, officeEmail=null, officePhone=null, editDirector=null, officeDirector=null, officeDirectorPhone=null, officeStaffNum=null, officeEmpNum=null, coverPicUrl=BTxjudbJDVO4PqdBR6On6Q==, journalPrice=null, startedYear=null, abbrevIsoEn=null, journalRemark=null, publicationField=null, 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