Ligand and Target Discovery by Fragment-Based Screening in Human Cells

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• 作者：Christopher G. Parker¹ ; ⁵ ; ^{cparker@scripps.edu} ; Andrea Galmozzi¹ ; ⁵ ; Yujia Wang¹ ; Bruno E. Correia² ; Kenji Sasaki¹ ; Christopher M. Joslyn¹ ; Arthur S. Kim¹ ; Cullen L. Cavallaro³ ; R. Michael Lawrence³ ; Stephen R. Johnson³ ; Iñ ; igo Narvaiza⁴ ; Enrique Saez¹ ; ^{esaez@scripps.edu} ; Benjamin F. Cravatt¹ ; ⁶ ; ^{cravatt@scripps.edu}
• 关键词：fragment-based ligand discovery ; FBLD ; chemical proteomics ; mass spectrometry ; photoreactivity ; phenotypic screening ; ligands ; chemical probes ; PGRMC2 ; adipogenesis
• 刊名：Cell
• 出版年：2017
• 出版时间：26 January 2017
• 年：2017
• 卷：168
• 期：3
• 页码：527-541.e29
• 全文大小：7802 K
• 卷排序：168

文摘

Chemical proteomics identifies numerous fragment-protein interactions in cells Interactions can be advanced into selective ligands that modulate protein function Fragment-based probes facilitate target identification in phenotypic screening Fragment-based ligands promote adipogenesis by stimulating PGRMC2 function