Proteomic discovery of chemical probes that perturb protein complexes in human cells.

activity-based protein profiling chemical probe covalent cysteine proteasome protein complexes proteomics size-exclusion chromatography spliceosome

Journal

Molecular cell
ISSN: 1097-4164
Titre abrégé: Mol Cell
Pays: United States
ID NLM: 9802571

Informations de publication

Date de publication:
18 05 2023
Historique:
received: 10 11 2021
revised: 09 01 2023
accepted: 28 03 2023
pmc-release: 18 05 2024
medline: 22 5 2023
pubmed: 22 4 2023
entrez: 21 04 2023
Statut: ppublish

Résumé

Most human proteins lack chemical probes, and several large-scale and generalizable small-molecule binding assays have been introduced to address this problem. How compounds discovered in such "binding-first" assays affect protein function, nonetheless, often remains unclear. Here, we describe a "function-first" proteomic strategy that uses size exclusion chromatography (SEC) to assess the global impact of electrophilic compounds on protein complexes in human cells. Integrating the SEC data with cysteine-directed activity-based protein profiling identifies changes in protein-protein interactions that are caused by site-specific liganding events, including the stereoselective engagement of cysteines in PSME1 and SF3B1 that disrupt the PA28 proteasome regulatory complex and stabilize a dynamic state of the spliceosome, respectively. Our findings thus show how multidimensional proteomic analysis of focused libraries of electrophilic compounds can expedite the discovery of chemical probes with site-specific functional effects on protein complexes in human cells.

Identifiants

pubmed: 37084731
pii: S1097-2765(23)00239-3
doi: 10.1016/j.molcel.2023.03.026
pmc: PMC10198961
mid: NIHMS1889442
pii:
doi:

Substances chimiques

Transcription Factors 0
Cysteine K848JZ4886
Ligands 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't Research Support, N.I.H., Extramural

Langues

eng

Sous-ensembles de citation

IM

Pagination

1725-1742.e12

Subventions

Organisme : NCI NIH HHS
ID : F32 CA265211
Pays : United States
Organisme : NCI NIH HHS
ID : R35 CA231991
Pays : United States
Organisme : NCI NIH HHS
ID : P30 CA008748
Pays : United States
Organisme : NHGRI NIH HHS
ID : U24 HG009889
Pays : United States
Organisme : NHGRI NIH HHS
ID : R01 HG004659
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA238249
Pays : United States
Organisme : Howard Hughes Medical Institute
ID : GT15176
Pays : United States

Commentaires et corrections

Type : CommentIn

Informations de copyright

Copyright © 2023 Elsevier Inc. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of interests G.M.S., V.F.V., and L.R.W. are employees of Vividion Therapeutics, and B.F.C. is a founder and member of the Board of Directors of Vividion Therapeutics. G.W.Y. is a co-founder, member of the Board of Directors, on the SAB, equity holder, and paid consultant for Locanabio and Eclipse BioInnovations. G.W.Y.’s interests have been reviewed and approved by the University of California, San Diego in accordance with its conflict-of-interest policies. A US provisional patent has been filed related to the work disclosed in this manuscript.

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Auteurs

Michael R Lazear (MR)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Jarrett R Remsberg (JR)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA. Electronic address: remsberg@scripps.edu.

Martin G Jaeger (MG)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Katherine Rothamel (K)

Department of Cellular and Molecular Medicine, University of California, San Diego, La Jolla, CA, USA.

Hsuan-Lin Her (HL)

Department of Cellular and Molecular Medicine, University of California, San Diego, La Jolla, CA, USA.

Kristen E DeMeester (KE)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Evert Njomen (E)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Simon J Hogg (SJ)

Human Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA.

Jahan Rahman (J)

Human Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA.

Landon R Whitby (LR)

Vividion Therapeutics, 5820 Nancy Ridge Drive, San Diego, CA 92121, USA.

Sang Joon Won (SJ)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Michael A Schafroth (MA)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Daisuke Ogasawara (D)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Minoru Yokoyama (M)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Garrett L Lindsey (GL)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Haoxin Li (H)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Jason Germain (J)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Sabrina Barbas (S)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Joan Vaughan (J)

Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, La Jolla, CA, USA.

Thomas W Hanigan (TW)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Vincent F Vartabedian (VF)

Department of Immunology and Microbiology, Scripps Research, La Jolla, CA 92037, USA.

Christopher J Reinhardt (CJ)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Melissa M Dix (MM)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA.

Seong Joo Koo (SJ)

Molecular and Cellular Pharmacology, Discovery Technologies and Molecular Pharmacology, Janssen Research and Development, Turnhoutseweg 30, 2340 Beerse, Belgium.

Inha Heo (I)

Molecular and Cellular Pharmacology, Discovery Technologies and Molecular Pharmacology, Janssen Research and Development, Turnhoutseweg 30, 2340 Beerse, Belgium.

John R Teijaro (JR)

Department of Immunology and Microbiology, Scripps Research, La Jolla, CA 92037, USA.

Gabriel M Simon (GM)

Vividion Therapeutics, 5820 Nancy Ridge Drive, San Diego, CA 92121, USA.

Brahma Ghosh (B)

Discovery Chemistry, Janssen Research & Development, Spring House, PA 19477, USA.

Omar Abdel-Wahab (O)

Human Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA.

Kay Ahn (K)

Molecular and Cellular Pharmacology, Discovery Technologies and Molecular Pharmacology, Janssen Research and Development, Spring House, PA 19477, USA.

Alan Saghatelian (A)

Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, La Jolla, CA, USA.

Bruno Melillo (B)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA; Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02142, USA.

Stuart L Schreiber (SL)

Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02142, USA; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA.

Gene W Yeo (GW)

Department of Cellular and Molecular Medicine, University of California, San Diego, La Jolla, CA, USA.

Benjamin F Cravatt (BF)

Department of Chemistry, Scripps Research, La Jolla, CA 92037, USA. Electronic address: cravatt@scripps.edu.

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Classifications MeSH