Ontology highlight
ABSTRACT:
SUBMITTER: Kok BP
PROVIDER: S-EPMC7442688 | biostudies-literature | 2020 Sep
REPOSITORIES: biostudies-literature
Kok Bernard P BP Ghimire Srijana S Kim Woojoo W Chatterjee Shreyosree S Johns Tyler T Kitamura Seiya S Eberhardt Jerome J Ogasawara Daisuke D Xu Janice J Sukiasyan Ara A Kim Sean M SM Godio Cristina C Bittencourt Julia M JM Cameron Michael M Galmozzi Andrea A Forli Stefano S Wolan Dennis W DW Cravatt Benjamin F BF Boger Dale L DL Saez Enrique E
Nature chemical biology 20200608 9
Activity-based protein profiling (ABPP) has been used extensively to discover and optimize selective inhibitors of enzymes. Here, we show that ABPP can also be implemented to identify the converse-small-molecule enzyme activators. Using a kinetically controlled, fluorescence polarization-ABPP assay, we identify compounds that stimulate the activity of LYPLAL1-a poorly characterized serine hydrolase with complex genetic links to human metabolic traits. We apply ABPP-guided medicinal chemistry to ...[more]