Intracellular Protein-Drug Interactions Probed by Direct Mass Spectrometry of Cell Lysates.

analytical methods drug discovery drug screening mass spectrometry protein analysis

Journal

Angewandte Chemie (International ed. in English)
ISSN: 1521-3773
Titre abrégé: Angew Chem Int Ed Engl
Pays: Germany
ID NLM: 0370543

Informations de publication

Date de publication:
01 09 2021
Historique:
revised: 23 05 2021
received: 11 04 2021
pubmed: 9 6 2021
medline: 4 11 2021
entrez: 8 6 2021
Statut: ppublish

Résumé

Understanding protein-ligand interactions in a cellular context is an important goal in molecular biology and biochemistry, and particularly for drug development. Investigators must demonstrate that drugs penetrate cells and specifically bind their targets. Towards that end, we present a native mass spectrometry (MS)-based method for analyzing drug uptake and target engagement in eukaryotic cells. This method is based on our previously introduced direct-MS method for rapid analysis of proteins directly from crude samples. Here, direct-MS enables label-free studies of protein-drug binding in human cells and is used to determine binding affinities of lead compounds in crude samples. We anticipate that this method will enable the application of native MS to a range of problems where cellular context is important, including protein-protein interactions, drug uptake and binding, and characterization of therapeutic proteins.

Identifiants

pubmed: 34101963
doi: 10.1002/anie.202104947
pmc: PMC8457057
doi:

Substances chimiques

Ligands 0
Pharmaceutical Preparations 0
Proteins 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

19637-19642

Informations de copyright

© 2021 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH.

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Auteurs

Rivkah Rogawski (R)

Department of Biomolecular Sciences, Weizmann Institute of Science, Rehovot, 7610001, Israel.

Adi Rogel (A)

Department of Chemical and Structural Biology, Weizmann Institute of Science, Rehovot, 7610001, Israel.

Itai Bloch (I)

Biotechnology Department, MIGAL-Galilee Research Institute, Kiryat-Shmona, 11016, Israel.

Maayan Gal (M)

Department of Oral Biology, The Goldschleger School of Dental Medicine, Sackler Faculty of Medicine, Tel Aviv University, Tel Aviv, 6997801, Israel.

Amnon Horovitz (A)

Department of Chemical and Structural Biology, Weizmann Institute of Science, Rehovot, 7610001, Israel.

Nir London (N)

Department of Chemical and Structural Biology, Weizmann Institute of Science, Rehovot, 7610001, Israel.

Michal Sharon (M)

Department of Biomolecular Sciences, Weizmann Institute of Science, Rehovot, 7610001, Israel.

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Classifications MeSH