| Structural highlights
3u4u is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: | ,
| | Gene: | CSNK2A1, CK2A1 (HUMAN) |
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Publication Abstract from PubMed
In this paper we describe a series of 3-cyano-5-aryl-7-aminopyrazolo[1,5-a]pyrimidine hits identified by kinase-focused subset screening as starting points for the structure-based design of conformationally constrained 6-acetamido-indole inhibitors of CK2. The synthesis, SAR, and effects of this novel series on Akt signaling and cell proliferation in vitro are described.
Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.,Dowling JE, Chuaqui C, Pontz TW, Lyne PD, Larsen NA, Block MH, Chen H, Su N, Wu A, Russell D, Pollard H, Lee JW, Peng B, Thakur K, Ye Q, Zhang T, Brassil P, Racicot V, Bao L, Denz CR, Cooke E ACS Med Chem Lett. 2012 Jan 24;3(4):278-83. doi: 10.1021/ml200257n. eCollection, 2012 Apr 12. PMID:24900464[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Dowling JE, Chuaqui C, Pontz TW, Lyne PD, Larsen NA, Block MH, Chen H, Su N, Wu A, Russell D, Pollard H, Lee JW, Peng B, Thakur K, Ye Q, Zhang T, Brassil P, Racicot V, Bao L, Denz CR, Cooke E. Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization. ACS Med Chem Lett. 2012 Jan 24;3(4):278-83. doi: 10.1021/ml200257n. eCollection, 2012 Apr 12. PMID:24900464 doi:http://dx.doi.org/10.1021/ml200257n
|
