1v1k | pdb_00001v1k
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| 1v1k, resolution 2.31Å | |||||||||||||
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| Sites: | AC1 | ||||||||||||
| Ligands: | ACE and 3FP | ||||||||||||
| Activity: | Transferred entry: 2.7.11.1, with EC number 2.7.1.37 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
CDK2 IN COMPLEX WITH A DISUBSTITUTED 4, 6-BIS ANILINO PYRIMIDINE CDK4 INHIBITOR
Overview
Using a high-throughput screening campaign, we identified the 4,6-bis anilino pyrimidines as inhibitors of the cyclin-dependent kinase, CDK4. Herein we describe the further chemical modification and use of X-ray crystallography to develop potent and selective in vitro inhibitors of CDK4.
About this Structure
1V1K is a Single protein structure of sequence from Homo sapiens. This structure supersedes the now removed PDB entry 1H06. Full crystallographic information is available from OCA.
Reference
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines., Beattie JF, Breault GA, Ellston RP, Green S, Jewsbury PJ, Midgley CJ, Naven RT, Minshull CA, Pauptit RA, Tucker JA, Pease JE, Bioorg Med Chem Lett. 2003 Sep 15;13(18):2955-60. PMID:12941311
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