Structural highlights
Function
[KC1G3_HUMAN] Serine/threonine-protein kinase. Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. It can phosphorylate a large number of proteins. Participates in Wnt signaling. Regulates fast synaptic transmission mediated by glutamate (By similarity).
Publication Abstract from PubMed
Screening of the Amgen compound library led to the identification of 2-phenylamino-6-cyano-1H-benzimidazole 1a as a potent CK1 gamma inhibitor with excellent kinase selectivity and unprecedented CK1 isoform selectivity. Further structure-based optimization of this series resulted in the discovery of 1h which possessed good enzymatic and cellular potency, excellent CK1 isoform and kinase selectivity, and acceptable pharmacokinetic properties.
2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1gamma) inhibitors.,Hua Z, Huang X, Bregman H, Chakka N, DiMauro EF, Doherty EM, Goldstein J, Gunaydin H, Huang H, Mercede S, Newcomb J, Patel VF, Turci SM, Yan J, Wilson C, Martin MW Bioorg Med Chem Lett. 2012 Sep 1;22(17):5392-5. doi: 10.1016/j.bmcl.2012.07.046. , Epub 2012 Jul 20. PMID:22877629[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Hua Z, Huang X, Bregman H, Chakka N, DiMauro EF, Doherty EM, Goldstein J, Gunaydin H, Huang H, Mercede S, Newcomb J, Patel VF, Turci SM, Yan J, Wilson C, Martin MW. 2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1gamma) inhibitors. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5392-5. doi: 10.1016/j.bmcl.2012.07.046. , Epub 2012 Jul 20. PMID:22877629 doi:10.1016/j.bmcl.2012.07.046
