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

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

Journal of Medicinal Chemistry

10.1021/acs.jmedchem.8b00060

https://doi.org/10.1021/acs.jmedchem.8b00060

Jacek Kwiatkowski, Boping Liu, Doris Hui Ying Tee, Guoying Chen, Nur Huda Binte Ahmad, Yun Xuan Wong, Zhi Ying Poh, Shi Hua Ang, Eldwin Sum Wai Tan, Esther Ong, Nurul Dinie, Anders Poulsen, Vishal Pendharkar, Kanda Sangthongpitag, May Ann Lee, Sugunavathi D/O Sepramaniam, Soo Yei Ho, Joseph Cherian, Jeffrey Hill, Thomas Hugo Keller, Alvin Wei Hung

drug discovery

24 April 2018

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

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.

PublisherCopyrights

Agency for Science, Technology and Research (A*STAR) Joint Council grant 1231B105

https://oar.a-star.edu.sg/communities-collections/articles/14195

0022-2623
1520-4804

Experimental Drug Development Centre