3e8c

Crystal structures of the kinase domain of PKA in complex with ATP-competitive inhibitorsCrystal structures of the kinase domain of PKA in complex with ATP-competitive inhibitors

Structural highlights 3e8c is a 12 chain structure with sequence from Bos taurus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: NonStd Res: , Related: 3e87, 3e88, 3e8d, 3e8e Gene: PKA, PRKACA (Bos taurus) Activity: cAMP-dependent protein kinase, with EC number 2.7.11.11 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 AKT inhibitors containing an imidazopyridine aminofurazan scaffold have been optimized. We have previously disclosed identification of the AKT inhibitor GSK690693, which has been evaluated in clinical trials in cancer patients. Herein we describe recent efforts focusing on investigating a distinct region of this scaffold that have afforded compounds (30 and 32) with comparable activity profiles to that of GSK690693. Aminofurazans as potent inhibitors of AKT kinase.,Rouse MB, Seefeld MA, Leber JD, McNulty KC, Sun L, Miller WH, Zhang S, Minthorn EA, Concha NO, Choudhry AE, Schaber MD, Heerding DA Bioorg Med Chem Lett. 2009 Mar 1;19(5):1508-11. Epub 2009 Jan 9. PMID:19179070 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

spinqualitylabelsall models 3e8c, resolution 2.20Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image