Article ; Online: Discovery of a selective c-MET inhibitor with a novel binding mode.
Bioorganic & medicinal chemistry letters
2022 Volume 75, Page(s) 128948
Abstract: The c-MET receptor tyrosine kinase has received considerable attention as a cancer drug target yet there remains a need for inhibitors which are selective for c-MET and able to target emerging drug-resistant mutants. We report here the discovery, by ... ...
Abstract | The c-MET receptor tyrosine kinase has received considerable attention as a cancer drug target yet there remains a need for inhibitors which are selective for c-MET and able to target emerging drug-resistant mutants. We report here the discovery, by screening a DNA-encoded chemical library, of a highly selective c-MET inhibitor which was shown by X-ray crystallography to bind to the kinase in an unprecedented manner. These results represent a novel mode of inhibiting c-MET with a small molecule and may provide a route to targeting drug-resistant forms of the kinase whilst avoiding potential toxicity issues associated with broad kinome inhibition. |
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MeSH term(s) | Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; DNA ; Protein Kinase Inhibitors/chemistry ; Proto-Oncogene Proteins c-met ; Small Molecule Libraries/chemistry |
Chemical Substances | Antineoplastic Agents ; Protein Kinase Inhibitors ; Small Molecule Libraries ; DNA (9007-49-2) ; Proto-Oncogene Proteins c-met (EC 2.7.10.1) |
Language | English |
Publishing date | 2022-08-17 |
Publishing country | England |
Document type | Journal Article |
ZDB-ID | 1063195-1 |
ISSN | 1464-3405 ; 0960-894X |
ISSN (online) | 1464-3405 |
ISSN | 0960-894X |
DOI | 10.1016/j.bmcl.2022.128948 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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