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3eid
From Proteopedia
| 3eid, resolution 3.15Å () | |||||||||
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| Ligands: | |||||||||
| Gene: | CDK2 (Homo sapiens), CCNA2, CCN1, CCNA (Homo sapiens) | ||||||||
| Activity: | Cyclin-dependent kinase, with EC number 2.7.11.22 | ||||||||
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
Contents |
CDK2/CyclinA complexed with a pyrazolopyridazine inhibitor
A novel series of pyrazolo[1,5-b]pyridazines have been synthesized and identified as cyclin dependant kinase inhibitors potentially useful for the treatment of solid tumors. Modification of the hinge-binding amine or the C(2)- and C(6)-substitutions on the pyrazolopyridazine core provided potent inhibitors of CDK4 and demonstrated enzyme selectivity against VEGFR-2 and GSK3beta.
Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors., Stevens KL, Reno MJ, Alberti JB, Price DJ, Kane-Carson LS, Knick VB, Shewchuk LM, Hassell AM, Veal JM, Davis ST, Griffin RJ, Peel MR, Bioorg Med Chem Lett. 2008 Nov 1;18(21):5758-62. Epub 2008 Sep 24. PMID:18835709
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
3eid is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.
See Also
Reference
- Stevens KL, Reno MJ, Alberti JB, Price DJ, Kane-Carson LS, Knick VB, Shewchuk LM, Hassell AM, Veal JM, Davis ST, Griffin RJ, Peel MR. Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors. Bioorg Med Chem Lett. 2008 Nov 1;18(21):5758-62. Epub 2008 Sep 24. PMID:18835709 doi:10.1016/j.bmcl.2008.09.069
Categories: Cyclin-dependent kinase | Homo sapiens | Alberti, J. | Hassell, A. | Kane-Carson, L. | Knick, V. | Peel, M. | Price, D. | Reno, M. | Shewchuk, L. | Steven, K. | Veal, J. | Atp-binding | Cdk2 | Cell cycle | Cell division | Cyclin | Kinase | Mitosis | Nucleotide-binding | Nucleus | Phosphoprotein | Serine/threonine-protein kinase | Transferase | Transferase-cell cycle complex
