Structural highlights
Function
CSK2A_MAIZE Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. The alpha chain contains the catalytic site.
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
A series of macrocyclic derivatives has been designed and synthesized based on the X-ray co-crystal structures of pyrazolo[1,5-a] [1,3,5]triazines with corn CK2 (cCK2) protein. Bioassays demonstrated that these macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds are potent CK2 inhibitors with K(i) around 1.0 nM and strongly inhibit cancer cell growth with IC(50) as low as approximately 100 nM.
Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities.,Nie Z, Perretta C, Erickson P, Margosiak S, Lu J, Averill A, Almassy R, Chu S Bioorg Med Chem Lett. 2008 Jan 15;18(2):619-23. Epub 2007 Nov 28. PMID:18055206[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Nie Z, Perretta C, Erickson P, Margosiak S, Lu J, Averill A, Almassy R, Chu S. Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities. Bioorg Med Chem Lett. 2008 Jan 15;18(2):619-23. Epub 2007 Nov 28. PMID:18055206 doi:S0960-894X(07)01383-2
