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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...
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 |
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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 |
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