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Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P‑Loop Cysteine

SRC is a major regulator of many signaling pathways and contributes to cancer development. However, development of a selective SRC inhibitor has been challenging, and FDA-approved SRC inhibitors, dasatinib and bosutinib, are multitargeted kinase inhibitors. Here, we describe our efforts to develop a...

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Bibliographische Detailangaben
Veröffentlicht in:J Med Chem
Hauptverfasser: Du, Guangyan, Rao, Suman, Gurbani, Deepak, Henning, Nathaniel J., Jiang, Jie, Che, Jianwei, Yang, Annan, Ficarro, Scott B., Marto, Jarrod A., Aguirre, Andrew J., Sorger, Peter K., Westover, Kenneth D., Zhang, Tinghu, Gray, Nathanael S.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2020
Schlagworte:
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7493195/
https://ncbi.nlm.nih.gov/pubmed/31935084
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b01502
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