7-Azaindole: A Versatile Scaffold for Developing Kinase Inhibitors.

doi:10.1248/cpb.c17-00380

Paper

7-Azaindole: A Versatile Scaffold for Developing Kinase Inhibitors.

Published 2018 · T. Irie, M. Sawa

Chemical & pharmaceutical bulletin

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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.

Study Snapshot

7-azaindole is a versatile scaffold for developing kinase inhibitors, with potential applications in treating various cancers and autoimmune diseases.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

7-Azaindole: A Versatile Scaffold for Developing Kinase Inhibitors.

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