Mechanistic Modeling of Lys745 Sulfonylation in EGFR C797S Reveals Chemical Determinants for Inhibitor Activity and Discriminates Reversible from Irreversible Agents.


Journal

Journal of chemical information and modeling
ISSN: 1549-960X
Titre abrégé: J Chem Inf Model
Pays: United States
ID NLM: 101230060

Informations de publication

Date de publication:
27 02 2023
Historique:
pubmed: 11 2 2023
medline: 3 3 2023
entrez: 10 2 2023
Statut: ppublish

Résumé

Targeted covalent inhibitors hold promise for drug discovery, particularly for kinases. Targeting the catalytic lysine of epidermal growth factor receptor (EGFR) has attracted attention as a new strategy to overcome resistance due to the emergence of C797S mutation. Sulfonyl fluoride derivatives able to inhibit EGFR

Identifiants

pubmed: 36762429
doi: 10.1021/acs.jcim.2c01586
pmc: PMC9976278
doi:

Substances chimiques

ErbB Receptors EC 2.7.10.1
sulfuryl fluoride 64B59K7U6Q
Lysine K3Z4F929H6
Protein Kinase Inhibitors 0
EGFR protein, human EC 2.7.10.1

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

1301-1312

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Auteurs

Kemel Arafet (K)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parco Area delle Scienze 27/A, I- 43124 Parma, Italy.
BioComp Group, Institute of Advanced Materials (INAM), Universitat Jaume I, 12071 Castelló, Spain.

Laura Scalvini (L)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parco Area delle Scienze 27/A, I- 43124 Parma, Italy.

Francesca Galvani (F)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parco Area delle Scienze 27/A, I- 43124 Parma, Italy.

Sergio Martí (S)

BioComp Group, Institute of Advanced Materials (INAM), Universitat Jaume I, 12071 Castelló, Spain.

Vicent Moliner (V)

BioComp Group, Institute of Advanced Materials (INAM), Universitat Jaume I, 12071 Castelló, Spain.

Marco Mor (M)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parco Area delle Scienze 27/A, I- 43124 Parma, Italy.
Microbiome Research Hub, University of Parma, Parco Area delle Scienze 11/A, I-43124 Parma, Italy.

Alessio Lodola (A)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parco Area delle Scienze 27/A, I- 43124 Parma, Italy.

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Classifications MeSH