1. Academic Validation
  2. Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors

Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors

  • J Med Chem. 2018 May 24;61(10):4386-4396. doi: 10.1021/acs.jmedchem.8b00060.
Jacek Kwiatkowski 1 Boping Liu 1 Doris Hui Ying Tee 1 Guoying Chen 1 Nur Huda Binte Ahmad 1 Yun Xuan Wong 1 Zhi Ying Poh 1 Shi Hua Ang 1 Eldwin Sum Wai Tan 1 Esther Hq Ong 1 Nurul Dinie 1 Anders Poulsen 1 Vishal Pendharkar 1 Kanda Sangthongpitag 1 May Ann Lee 1 Sugunavathi Sepramaniam 1 Soo Yei Ho 1 Joseph Cherian 1 Jeffrey Hill 1 Thomas H Keller 1 Alvin W Hung 1
Affiliations

Affiliation

  • 1 Experimental Therapeutics Centre , Agency for Science, Technology and Research (A*STAR) , 11 Biopolis Way, Helios #03-10/11 , Singapore 138667 , Singapore.
Abstract

Protein kinase C iota (PKC-ι) is an atypical kinase implicated in the promotion of different Cancer types. A biochemical screen of a fragment library has identified several hits from which an azaindole-based scaffold was chosen for optimization. Driven by a structure-activity relationship and supported by molecular modeling, a weakly bound fragment was systematically grown into a potent and selective inhibitor against PKC-ι.

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