7-Azaindole: A Versatile Scaffold for Developing Kinase Inhibitors
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- Irie Takayuki
- Research and Development, Carna Biosciences, Inc.
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- Sawa Masaaki
- Research and Development, Carna Biosciences, Inc.
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Description
<p>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.</p>
Journal
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- Chemical and Pharmaceutical Bulletin
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Chemical and Pharmaceutical Bulletin 66 (1), 29-36, 2018
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390001204177933056
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- NII Article ID
- 130006301008
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- NII Book ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL BIB ID
- 028738733
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- PubMed
- 29311509
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed