2c6d
From Proteopedia
AURORA A KINASE ACTIVATED MUTANT (T287D) IN COMPLEX WITH ADPNP
Overview
A novel series of 5-aminopyrimidinyl quinazolines has been developed from anilino-quinazoline 1, which was identified in a high throughput screen for Aurora A. Introduction of the pyrimidine ring and optimisation of the substituents both on this ring and at the C7 position of the quinazoline led to the discovery of compounds that are highly specific Aurora kinase inhibitors. Co-crystallisation of one of these inhibitors with a fragment of Aurora A shows the importance of the benzamido group in achieving selectivity.
About this Structure
2C6D is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors., Heron NM, Anderson M, Blowers DP, Breed J, Eden JM, Green S, Hill GB, Johnson T, Jung FH, McMiken HH, Mortlock AA, Pannifer AD, Pauptit RA, Pink J, Roberts NJ, Rowsell S, Bioorg Med Chem Lett. 2006 Mar 1;16(5):1320-3. Epub 2005 Dec 5. PMID:16337122 Page seeded by OCA on Sat May 3 21:19:36 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Anderson, M. | Breed, J. | Mcmiken, H H.J. | Pannifer, A D. | Pauptit, R A. | Rowsell, S. | Atp-binding | Aurora | Cancer | Cell cycle | Kinase | Mitosis | Nucleotide-binding | Phosphorylation | Serine/threonine-protein kinase | Transferase
