Structural Basis for Targeting the Folded P-Loop Conformation of c-MET

[Image: see text] We report here a fragment screen directed toward the c-MET kinase from which we discovered a series of inhibitors able to bind to a rare conformation of the protein in which the P-loop adopts a collapsed, or folded, arrangement. Preliminary SAR exploration led to an inhibitor (7) w...

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Detalles Bibliográficos
Autores principales: Collie, Gavin W., Michaelides, Iacovos N., Embrey, Kevin, Stubbs, Christopher J., Börjesson, Ulf, Dale, Ian L., Snijder, Arjan, Barlind, Louise, Song, Kun, Khurana, Puneet, Phillips, Christopher, Storer, R. Ian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7812667/
https://www.ncbi.nlm.nih.gov/pubmed/33488978
http://dx.doi.org/10.1021/acsmedchemlett.0c00392

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7812667/
https://www.ncbi.nlm.nih.gov/pubmed/33488978
http://dx.doi.org/10.1021/acsmedchemlett.0c00392

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