4.7 Article

Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors

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JOURNAL OF MEDICINAL CHEMISTRY
卷 61, 期 10, 页码 4386-4396

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AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.8b00060

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  1. Agency for Science, Technology and Research (A*STAR) Joint Council grant [1231B105]

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Protein kinase C iota (PKC-i) is an atypical kinase implicated in the promotion of different cancer types. A biochemical screen of a fragment library has identified several hits from which an azaindole-based scaffold was chosen for optimization. Driven by a structure activity relationship and supported by molecular modeling, a weakly bound fragment was systematically grown into a potent and selective inhibitor against PKC-i.

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