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2. Key Lab of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Science of Lanzhou University, Lanzhou 730020, China;
3. National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Science, Shanghai 201203, China, fund=null, authors=GAO Wei1 , SHAO Wei2 , SU Gang2 , LI Jia3 , XIE Xiaodong2 , authorsList=GAO Wei, SHAO Wei, SU Gang, LI Jia, XIE Xiaodong), CN=ArticleExt(id=1242131577392673732, articleId=1242131574536348342, tenantId=1146029695717560320, journalId=1146031591421210625, language=CN, title=蛋白酪氨酸磷酸酶SHP2抑制剂高通量筛选模型的建立和应用, columnId=1146540929516700224, journalTitle=科技导报, columnName=研究论文, runingTitle=null, highlight=null, articleAbstract=为了建立体外蛋白酪氨酸磷酸酶SHP2抑制剂的高通量筛选模型,筛选潜在的SHP2抑制剂,通过应用大肠杆菌系统克隆表达GST-SHP2 融合蛋白,经过GST-Sepharose 亲和层析分离得到纯化的GST-SHP2 蛋白,建立384 孔板的高通量筛选模型,对48000个有明确结构的小分子化合物进行体外筛选,筛选出75个活性化合物对SHP2的抑制作用大于50%,确定3个化合物具有较高的抑制活性。该筛选模型灵敏、稳定,对SHP2抑制剂药物研发打下了基础。, correspAuthors=null, authorNote=高炜,主任医师,研究方向为肿瘤临床及肿瘤遗传学,电子信箱:329921879@qq.com, correspAuthorsNote=谢小冬,xdxie@lzu.edu.cn, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=zX/2uGKj+62HroCs8Rtkpg==, pdfFileSize=631125, 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=1. 兰州军区总医院普胸外科, 兰州 730050;
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科技导报
| 研究论文 2014, 32(4-5): 91-94
蛋白酪氨酸磷酸酶SHP2抑制剂高通量筛选模型的建立和应用
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高炜1 , 邵伟2 , 苏刚2 , 李佳3 , 谢小冬2
作者信息
1. 兰州军区总医院普胸外科, 兰州 730050;
2. 兰州大学基础医学院, 甘肃省新药临床前研究重点实验室, 兰州 730020;
3. 中国科学院上海药物研究所, 国家新药筛选中心, 上海 201203
通讯作者:
谢小冬,xdxie@lzu.edu.cn
Establishment and Application of High-throughput Screening Model for SHP Inhibitors
Affiliations
出版时间: 2014-02-08
doi: 10.3981/j.issn.1000-7857.2014.h1.015
文章导航
为了建立体外蛋白酪氨酸磷酸酶SHP2抑制剂的高通量筛选模型,筛选潜在的SHP2抑制剂,通过应用大肠杆菌系统克隆表达GST-SHP2 融合蛋白,经过GST-Sepharose 亲和层析分离得到纯化的GST-SHP2 蛋白,建立384 孔板的高通量筛选模型,对48000个有明确结构的小分子化合物进行体外筛选,筛选出75个活性化合物对SHP2的抑制作用大于50%,确定3个化合物具有较高的抑制活性。该筛选模型灵敏、稳定,对SHP2抑制剂药物研发打下了基础。
The aims of this study is to set up a high throughput screening model for SHP2 inhibitors and screen the potential inhibitors. By the E. coil expression system GST-SHP2 fusion protein is cloned and over expressed. High-purity SHP2 protein is purified though GSTSepharose column. After establishing the high through screening system with the colorimetric assay of SHP2, a library of 48000 pure compounds is screened using the 384 micro- plate. Among them 75 compounds have inhibitory effects over 50%. Ultimately, three inhibitors are identified as SHP2 inhibitors with high activity. The high throughput screening is a highly sensitive, inexpensive, and operationally simple assay method in identifying SHP2 inhibitors.
SHP2
/
inhibitor
/
high throughput screening
高炜, 邵伟, 苏刚, 李佳, 谢小冬.
蛋白酪氨酸磷酸酶SHP2抑制剂高通量筛选模型的建立和应用.
科技导报,
2014
, 32
(4-5)
: 91
-94
.
DOI: 10.3981/j.issn.1000-7857.2014.h1.015
GAO Wei, SHAO Wei, SU Gang, LI Jia, XIE Xiaodong.
Establishment and Application of High-throughput Screening Model for SHP Inhibitors[J].
Science & Technology Review ,
2014
, 32
(4-5)
: 91
-94
.
DOI: 10.3981/j.issn.1000-7857.2014.h1.015
2014年第32卷第4-5期
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文章信息
doi: 10.3981/j.issn.1000-7857.2014.h1.015
接收时间:2013-08-10
首发时间:2014-04-09
出版时间:2014-02-08
收稿日期:2013-08-10
修回日期:2013-11-30
通讯作者:
谢小冬,xdxie@lzu.edu.cn
https://castjournals.cast.org.cn/joweb/kjdb/CN/10.3981/j.issn.1000-7857.2014.h1.015
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2种不同金属材料的力学参数
科 Family 属数 Number of genus 种数 Number of species 占总种数比例 Percentage of total species (%) 属 Genus 种数 Number of species 占总种数比例 Percentage of total species (%) 鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78 小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39 多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39 红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87 小菇属 Mycena 11 5.26 光柄菇属 Pluteus 5 2.39 红菇属 Russula 17 8.13 栓菌属 Trametes 5 2.39
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