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Determining cysteines available for covalent inhibition across the human kinome

Covalently bound protein kinase inhibitors have been frequently designed to target non-catalytic cysteines at the ATP binding site. Thus, it is important to know if a given cysteine can form a covalent bond. Here we combine a function-site interaction fingerprint method and DFT calculations to deter...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Zhao, Zheng, Liu, Qingsong, Bliven, Spencer, Xie, Lei, Bourne, Philip E.
Formato: Artigo
Idioma:Inglês
Publicado em: 2017
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5493210/
https://ncbi.nlm.nih.gov/pubmed/28326775
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01815
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