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• W2776128170 abstract "The majority of kinase inhibitors have been developed as ATP competitors to interact with a hinge region in ATP binding sites of kinases. 7-Azaindole has been found as an excellent hinge binding motif by making two hydrogen bonds with the kinase hinge region. Vemurafenib, a B-RAF kinase (serine–threonine kinase [STK]) inhibitor approved by the U.S. Food and Drug Administration (FDA) for the treatment of melanoma, was created from this simple 7-azaindole fragment by successful use of structure-based drug design techniques. The huge potential of 7-azaindole as a hinge-binding motif has encouraged many researchers to employ it as a kinase privileged fragment. This paper will review recent examples of 7-azaindole-based kinase inhibitors, and discusses their binding interactions with the kinase hinge regions." @default.
• W2776128170 created "2018-01-05" @default.
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• W2776128170 date "2018-01-01" @default.
• W2776128170 modified "2023-10-17" @default.
• W2776128170 title "7-Azaindole: A Versatile Scaffold for Developing Kinase Inhibitors" @default.
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• W2776128170 doi "https://doi.org/10.1248/cpb.c17-00380" @default.
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