Molecular Basis of c-MET Inhibition by Approved Small Molecule Drugs: A Structural Perspective

ACS Medicinal Chemistry Letters 2026 Open access

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Authors: Isabella C. Russell, Paulina Bachurska-Szpala, Lotte van Beek, Iacovos N. Michaelides, Christopher Phillips, Arjan Snijder, Christopher J. Stubbs, Gavin W. Collie
DOI: 10.1021/acsmedchemlett.5c00713
Cited by: 4
References: 43

Abstract

The c-MET kinase is a driver of many cancers, and as such, there are a number of small molecule inhibitors of this kinase approved for clinical use. In this Microperspective, we provide a structural overview of the molecular basis by which these drugs inhibit c-MET, focusing on key features contributing to activity, selectivity, and drug resistance. Where necessary, relevant crystal structures not publicly available were determined and are discussed here alongside existing structural data.

Fields of Study & Subjects

Melanoma and MAPK Pathways Organic Chemistry Cycloaddition Reactions Photochromic and Fluorescence Chemistry

Publication details

Journal / source
ACS Medicinal Chemistry Letters
Publisher
American Chemical Society (ACS)
Volume
17
Issue
3
Pages
590–597
Publication date
6 February 2026
Language
EN