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An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells.
Vinogradova, Ekaterina V; Zhang, Xiaoyu; Remillard, David; Lazar, Daniel C; Suciu, Radu M; Wang, Yujia; Bianco, Giulia; Yamashita, Yu; Crowley, Vincent M; Schafroth, Michael A; Yokoyama, Minoru; Konrad, David B; Lum, Kenneth M; Simon, Gabriel M; Kemper, Esther K; Lazear, Michael R; Yin, Sifei; Blewett, Megan M; Dix, Melissa M; Nguyen, Nhan; Shokhirev, Maxim N; Chin, Emily N; Lairson, Luke L; Melillo, Bruno; Schreiber, Stuart L; Forli, Stefano; Teijaro, John R; Cravatt, Benjamin F.
Affiliation
  • Vinogradova EV; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA. Electronic address: vinograd@scripps.edu.
  • Zhang X; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Remillard D; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Lazar DC; Department of Immunology and Infectious Disease, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Suciu RM; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Wang Y; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Bianco G; Department of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Yamashita Y; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA; Medicinal Chemistry Research Laboratories, New Drug Research Division, Otsuka Pharmaceutical Co., Ltd., 463-10 Kawauchi-cho, Tokushima 771-0192, Japan.
  • Crowley VM; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Schafroth MA; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Yokoyama M; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Konrad DB; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Lum KM; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Simon GM; Vividion Therapeutics, 5820 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Kemper EK; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Lazear MR; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Yin S; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Blewett MM; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Dix MM; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Nguyen N; Department of Immunology and Infectious Disease, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Shokhirev MN; Razavi Newman Integrative Genomics and Bioinformatics Core, The Salk Institute for Biological Studies, La Jolla, CA 92037, USA.
  • Chin EN; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Lairson LL; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Melillo B; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA; Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02138, USA.
  • Schreiber SL; Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02138, USA; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA.
  • Forli S; Department of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Teijaro JR; Department of Immunology and Infectious Disease, The Scripps Research Institute, La Jolla, CA 92037, USA. Electronic address: teijaro@scripps.edu.
  • Cravatt BF; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA. Electronic address: cravatt@scripps.edu.
Cell ; 182(4): 1009-1026.e29, 2020 08 20.
Article in En | MEDLINE | ID: mdl-32730809
Electrophilic compounds originating from nature or chemical synthesis have profound effects on immune cells. These compounds are thought to act by cysteine modification to alter the functions of immune-relevant proteins; however, our understanding of electrophile-sensitive cysteines in the human immune proteome remains limited. Here, we present a global map of cysteines in primary human T cells that are susceptible to covalent modification by electrophilic small molecules. More than 3,000 covalently liganded cysteines were found on functionally and structurally diverse proteins, including many that play fundamental roles in immunology. We further show that electrophilic compounds can impair T cell activation by distinct mechanisms involving the direct functional perturbation and/or degradation of proteins. Our findings reveal a rich content of ligandable cysteines in human T cells and point to electrophilic small molecules as a fertile source for chemical probes and ultimately therapeutics that modulate immunological processes and their associated disorders.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: T-Lymphocytes / Cysteine / Ligands Limits: Humans Language: En Journal: Cell Year: 2020 Type: Article

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: T-Lymphocytes / Cysteine / Ligands Limits: Humans Language: En Journal: Cell Year: 2020 Type: Article