| Structural highlights
1p2a is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: |
| | Related: | 1fvt |
| Gene: | CDK2 (Homo sapiens) |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
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 novel class of 3,5,6-trisubstituted naphthostyril analogues was designed and synthesized to study the structure-activity relationship for inhibition of cyclin-dependent kinase 2 (CDK2). These compounds, particularly molecules with side-chain modifications providing additional hydrogen bonding capability, were demonstrated to be potent CDK2 inhibitors with cellular activities consistent with CDK2 inhibition. These molecules inhibited tumor cell proliferation and G1-S and G2-M cell-cycle progression in vitro. The X-ray crystal structure of a 2-aminoethyleneamine derivative bound to CDK2, refined to 2.5A resolution, is presented.
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.,Liu JJ, Dermatakis A, Lukacs C, Konzelmann F, Chen Y, Kammlott U, Depinto W, Yang H, Yin X, Chen Y, Schutt A, Simcox ME, Luk KC Bioorg Med Chem Lett. 2003 Aug 4;13(15):2465-8. PMID:12852944[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Liu JJ, Dermatakis A, Lukacs C, Konzelmann F, Chen Y, Kammlott U, Depinto W, Yang H, Yin X, Chen Y, Schutt A, Simcox ME, Luk KC. 3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors. Bioorg Med Chem Lett. 2003 Aug 4;13(15):2465-8. PMID:12852944
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