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Kee, Jung-Min
Bioorganic and Chembio Lab
Research Interests
  • Chemical biology, organic synthesis, peptide chemistry, synthetic protein chemistry

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Function through bio-inspired, synthesis-informed design: step-economical syntheses of designed kinase inhibitors

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Title
Function through bio-inspired, synthesis-informed design: step-economical syntheses of designed kinase inhibitors
Author
Wender, Paul A.Axtman, Alison D.Golden, Jennifer E.Kee, Jung-MinSirois, Lauren E.Quiroz, Ryan V.Stevens, Matthew C.
Issue Date
2014-12
Publisher
Royal Society of Chemistry
Citation
ORGANIC CHEMISTRY FRONTIERS, v.1, no.10, pp.1166 - 1171
Abstract
The human kinome comprises over 500 protein kinases. When mutated or over-expressed, many play critical roles in abnormal cellular functions associated with cancer, cardiovascular disease and neurological disorders. Here we report a step-economical approach to designed kinase inhibitors inspired by the potent, but non-selective, natural product staurosporine, and synthetically enabled by a novel, complexity-increasing, serialized [5 + 2]/[4 + 2] cycloaddition strategy. This function-oriented synthesis approach rapidly affords tunable scaffolds, and produced a low nanomolar inhibitor of protein kinase C.
URI
https://scholarworks.unist.ac.kr/handle/201301/10810
URL
http://pubs.rsc.org/en/Content/ArticleLanding/2014/QO/C4QO00228H#!divAbstract
DOI
10.1039/c4qo00228h
ISSN
2052-4129
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CHM_Journal Papers
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