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3E87

Crystal structures of the kinase domain of AKT2 in complex with ATP-competitive inhibitors

Summary for 3E87
Entry DOI10.2210/pdb3e87/pdb
Related3E88 3E8C 3E8D 3E8E
DescriptorRAC-beta serine/threonine-protein kinase, Glycogen synthase kinase-3 beta peptide, N-[(1S)-2-amino-1-phenylethyl]-5-(1H-pyrrolo[2,3-b]pyridin-4-yl)thiophene-2-carboxamide, ... (4 entities in total)
Functional Keywordsakt2, kinase, gsk3 beta, atp-binding, nucleotide-binding, phosphoprotein, serine/threonine-protein kinase, transferase, wnt signaling pathway
Biological sourceHomo sapiens (human)
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Cellular locationCytoplasm: P31751 P49841
Total number of polymer chains4
Total formula weight81116.36
Authors
Concha, N.O.,Elkins, P.A.,Smallwood, A.,Ward, P. (deposition date: 2008-08-19, release date: 2008-10-14, Last modification date: 2024-11-20)
Primary citationRouse, M.B.,Seefeld, M.A.,Leber, J.D.,McNulty, K.C.,Sun, L.,Miller, W.H.,Zhang, S.,Minthorn, E.A.,Concha, N.O.,Choudhry, A.E.,Schaber, M.D.,Heerding, D.A.
Aminofurazans as potent inhibitors of AKT kinase
Bioorg.Med.Chem.Lett., 19:1508-1511, 2009
Cited by
PubMed Abstract: 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.
PubMed: 19179070
DOI: 10.1016/j.bmcl.2009.01.002
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.3 Å)
Structure validation

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