Fragment-based drug discovery of potent Protein Kinase C-iota inhibitors

Fragment-based drug discovery of potent Protein Kinase C-iota inhibitors
Title:
Fragment-based drug discovery of potent Protein Kinase C-iota inhibitors
Other Titles:
Journal of Medicinal Chemistry
DOI:
10.1021/acs.jmedchem.8b00060
Publication Date:
24 April 2018
Citation:
Dharmesh Kumar, Sridhar Idapalapati, Wang Wei, Microstructural Response and Strain Hardening in Deep Cold Rolled Nickel-based Superalloy for Aerospace Application, Procedia CIRP, Volume 71, 2018, Pages 374-379, ISSN 2212-8271, https://doi.org/10.1016/j.procir.2018.05.044.0022-2623
Abstract:
Protein Kinase C iota (PKC-i) is an atypical kinase implicated in the promotion of different cancer types. A biochemical screen of fragment library has identified several hits, from which an azaindole-based scaffold was chosen for optimization. Driven by structure-activity relationship and supported by molecular modelling, a weakly bound fragment was systematically grown into a potent and selective inhibitor against PKC-i.
License type:
PublisherCopyrights
Funding Info:
Agency for Science, Technology and Research (A*STAR) Joint Council grant 1231B105
Description:
ISSN:
0022-2623
1520-4804
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