收藏本站
《中国生物化学与分子生物学会第十二届全国会员代表大会暨2018年全国学术会议摘要集》2018年
收藏 | 手机打开
二维码
手机客户端打开本文

Accelerating the throughput of affinity mass spectrometry-based ligand screening towards G-protein coupled receptors

Yan Lu  Shanshan Qin  Wenqing Shui  
【摘要】:As an important transmembrane signaling modulator,G protein-coupled receptors(GPCRs) account for more than 30% of the marketed drugs.To investigate ligand specificity to GPCRs,protein-ligand interaction can be analyzed by various technologies,such as SPR,NMR,ITC,etc.In recent years,affinity mass spectrometry(MS)-based platforms have gained increasing success in drug discovery mostly towards soluble protein targets.However,transmembrane proteins,especially GPCRs,remain challenging targets for affinity MS screening.We have previously established an efficient workflow for ligand screening towards GPCRs embedded in cell membranes1.In this study,we present another approach adapted to ligand screening towards purified receptor targets.The throughput of our GPCR ligand screening platform has been significantly accelerated by pooling tens of thousands of compounds in one mixture.High-affinity ligands were repeatedly identified when we compared the hits from screening 2 K compounds up to 20 K compounds in one cocktail.Several new antagonists for adenosine 2 A receptor have been discovered using our affinity MS ligand screens combined with cell activity assays,which demonstrates the high efficiency and reduced cost of our integrated platform for discovery of GPCR modulators.

【相似文献】
中国期刊全文数据库 前10条
1 ;β_2-Adrenoceptor affinity chromatography and its application in the screening of the active compounds from Semen Armeniacae Amarum[J];Chinese Science Bulletin;2008年06期
2 Hua-Jun Gao;Ya-Jing Chen;Duo Zuo;Ming-Ming Xiao;Ying Li;Hua Guo;Ning Zhang;Rui-Bing Chen;;Quantitative proteomic analysis for high-throughput screening of differential glycoproteins in hepatocellular carcinoma serum[J];Cancer Biology & Medicine;2015年03期
3 ;New approach for screening anti-tumor compounds[J];Chinese Science Bulletin;2003年07期
4 ;Establishment of a high-throughput screening system for universal anti-HIV targets[J];Chinese Science Bulletin;2010年10期
5 ;Immobilized enzyme reactors in HPLC and its application in inhibitor screening:A review[J];Journal of Pharmaceutical Analysis;2012年02期
6 ;Perfect high throughput screening assay: a crucial technique for drug discovery[J];Acta Pharmacologica Sinica;2005年10期
7 FAN B.T.,A. PANAYE,J-P. DOUCET;Virtual Screening and Structure Generation Applied to Drug Design[J];合成化学;2004年S1期
8 ;Application of surface plasmon resonance in screening adsorbents and explaining adsorption phenomena using model polymers[J];Chinese Science Bulletin;2010年32期
9 Weidong Liu;Chuanliu Wu;;A mini-review and perspective on multicyclic peptide mimics of antibodies[J];Chinese Chemical Letters;2018年07期
10 ;Con A affinity glycoproteomics of normal human liver tissue[J];Science in China(Series C:Life Sciences);2007年03期
中国重要会议论文全文数据库 前10条
1 Yan Lu;Shanshan Qin;Wenqing Shui;;Accelerating the throughput of affinity mass spectrometry-based ligand screening towards G-protein coupled receptors[A];中国生物化学与分子生物学会第十二届全国会员代表大会暨2018年全国学术会议摘要集[C];2018年
2 ;High-throughput screening for protein tyrosine kinases inhibitors[A];中国药理学会第十一次全国学术会议专刊[C];2011年
3 Jinzeng Wang;;High throughput drug screening technology and its application[A];第五届全国生物信息学与系统生物学学术大会论文集[C];2012年
4 Jiang-Feng Yuan;Zhi-Qi Zhang;;Cell Affinity Capture and HPLC-MS Analysis for Anticardiovascular Diseases Drug Screening from Danshen[A];第二十届全国色谱学术报告会及仪器展览会论文集(第三分册)[C];2015年
5 周庆同;赵素文;;Understanding GPCR diversity and ligand specificity from the big data in virtual screening[A];中国化学会-生物物理化学专业委员会第四届全国生物物理化学会议论文集[C];2016年
6 Michael X.Zhu;;High throughput screening of novel inhibitors for TRPC4/C5 channels[A];中国神经科学学会第九届全国学术会议暨第五次会员代表大会论文摘要集[C];2011年
7 周越洋;吴方;;High throughput drug screening model and enzyme modulators[A];中国生物化学与分子生物学会第十一次会员代表大会暨2014年全国学术会议论文集——专题报告七[C];2014年
8 De-Sheng Pei;;Anti-tumor ingredients screening from natural medicine using zebrafish xenograft model[A];第十四届全国中药和天然药物学术研讨会论文摘要[C];2014年
9 谢俊岭;赫慧文;陈翀;白鹂鹏;刘妍;王威;曹峰琦;吴鹏;罗云萍;;High-throughput RNAi screening reveals novel inflammationrelated modulators of CSC identity[A];第九届全国免疫学学术大会论文集[C];2014年
10 杨学刚;陈端;薛英;;Integration of ligand-based and structure-based approaches for prediction and screening of factor Xa inhibitors[A];第四届全国生物信息学与系统生物学学术大会论文集[C];2010年
中国博士学位论文全文数据库 前1条
1 杨健;面向具有统计QoS保障的无线网络容量域分析和资源分配[D];西安电子科技大学;2016年
中国硕士学位论文全文数据库 前4条
1 SHAILENDRA SHAH;[D];重庆医科大学;2016年
2 Kien Thi Xuan Dao(坚氏春桃);[D];华东理工大学;2014年
3 SHAZLY ALSOLIBY;人工免疫杂交学习方法及其在函数近似中的应用[D];南昌大学;2007年
4 SAPHALTA SHRESTHA;中国境内女大学生乳腺癌知识—态度—行为调查的横断面研究[D];天津医科大学;2013年
 快捷付款方式  订购知网充值卡  订购热线  帮助中心
  • 400-819-9993
  • 010-62791813
  • 010-62985026