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A Structure-guided Approach to Creating Covalent FGFR Inhibitors

The fibroblast growth factor receptor tyrosine kinases (FGFR1, 2, 3, and 4) represent promising therapeutic targets in a number of cancers. We have developed the first potent and selective irreversible inhibitor of FGFR1, 2, 3, and 4 which we named FIIN-1 that forms a covalent bond with cysteine 486...

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Detalhes bibliográficos
Main Authors: Zhou, Wenjun, Hur, Wooyoung, McDermott, Ultan, Dutt, Amit, Xian, Wa, Picarro, Scott B., Zhang, Jianming, Sharma, Sreenath V., Brugge, Joan, Meyerson, Matthew, Settleman, Jeffrey, Gray, Nathanael S.
Formato: Artigo
Idioma:Inglês
Publicado em: 2010
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC2920453/
https://ncbi.nlm.nih.gov/pubmed/20338520
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.chembiol.2010.02.007
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