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Acquisition of a Group A-selective Src Kinase Inhibitor via a Global Targeting Strategy

Title
Acquisition of a Group A-selective Src Kinase Inhibitor via a Global Targeting Strategy
Author
하정미
Issue Date
2006-05
Publisher
AMER CHEMICAL SOC
Citation
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, v. 128, No. 18, Page. 5996-5997
Abstract
A “global” strategy for the acquisition of selective high affinity inhibitors for the Src kinase subfamily of tyrosine kinases is described. Members of the Src family exhibit a strong amino acid sequence homology. However, recent studies have revealed differences in the relative spatial relationships of the three distinct protein-binding domains present in these enzymes. We have constructed an inhibitor, using an amalgamation of combinatorial methods and directed design, which simultaneously associates with the active site and an ancillary protein-binding region (SH2 domain). The inhibitor exhibits high inhibitory potency and selectivity for the Group A versus Group B subset of Src kinases.
URI
https://pubs.acs.org/doi/abs/10.1021/ja060136ihttp://repository.hanyang.ac.kr/handle/20.500.11754/107873
ISSN
0002-7863
DOI
10.1021/ja060136i
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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