Abstract

The ability to characterize entire classes of proteins based on activity would greatly accelerate both the assignment of protein function in the genome era and the identification of new biomarl

Public Health Relevance

A large fraction of human enzymes remain uncharacterized in terms of their function in health and disease. We have developed advanced chemical technologies to functionally characterize enzymes directly in native biological systems. The goal of this application is to further develop and apply these technologies to identify enzymes that play important roles in cancer, which may serve as valuable new biomarkers and therapeutic targets.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Cancer Institute (NCI)
Type
Method to Extend Research in Time (MERIT) Award (R37)
Project #
5R37CA087660-16
Application #
8822844
Study Section
Special Emphasis Panel (NSS)
Program Officer
Fu, Yali
Project Start
2014-03-01
Project End
2019-02-28
Budget Start
2015-03-01
Budget End
2016-02-29
Support Year
16
Fiscal Year
2015
Total Cost
$294,818
Indirect Cost
$139,241

  Institution

Name
Scripps Research Institute
Department
Type
DUNS #
781613492
City
La Jolla
State
CA
Country
United States
Zip Code
92037

  Publications

Hacker, Stephan M; Backus, Keriann M; Lazear, Michael R et al. (2017) Global profiling of lysine reactivity and ligandability in the human proteome. Nat Chem 9:1181-1190
Bar-Peled, Liron; Kemper, Esther K; Suciu, Radu M et al. (2017) Chemical Proteomics Identifies Druggable Vulnerabilities in a Genetically Defined Cancer. Cell 171:696-709.e23
Whitby, Landon R; Obach, R Scott; Simon, Gabriel M et al. (2017) Quantitative Chemical Proteomic Profiling of the in Vivo Targets of Reactive Drug Metabolites. ACS Chem Biol 12:2040-2050
Guo, Chun-Jun; Chang, Fang-Yuan; Wyche, Thomas P et al. (2017) Discovery of Reactive Microbiota-Derived Metabolites that Inhibit Host Proteases. Cell 168:517-526.e18
Niessen, Sherry; Dix, Melissa M; Barbas, Sabrina et al. (2017) Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors. Cell Chem Biol 24:1388-1400.e7
Chen, Ying-Chu; Backus, Keriann M; Merkulova, Maria et al. (2017) Covalent Modulators of the Vacuolar ATPase. J Am Chem Soc 139:639-642
Briggs, Kimberly J; Koivunen, Peppi; Cao, Shugeng et al. (2016) Paracrine Induction of HIF by Glutamate in Breast Cancer: EglN1 Senses Cysteine. Cell 166:126-39
Chen, Wentao; Dong, Jiajia; Plate, Lars et al. (2016) Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(s) through Chemoselective SuFEx Reaction with a Binding Site Tyr Residue. J Am Chem Soc 138:7353-64
Zaro, Balyn W; Whitby, Landon R; Lum, Kenneth M et al. (2016) Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors. J Am Chem Soc 138:15841-15844
Dugan, Amanda; Majmudar, Chinmay Y; Pricer, Rachel et al. (2016) Discovery of Enzymatic Targets of Transcriptional Activators via in Vivo Covalent Chemical Capture. J Am Chem Soc 138:12629-35

Showing the most recent 10 out of 76 publications