2gu8
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(New page: 200px<br /><applet load="2gu8" size="350" color="white" frame="true" align="right" spinBox="true" caption="2gu8, resolution 2.20Å" /> '''Discovery of 2-Pyrim...)
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Revision as of 13:26, 23 January 2008
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Discovery of 2-Pyrimidyl-5-Amidothiophenes as Novel and Potent Inhibitors for AKT: Synthesis and SAR Studies
Overview
A series of 2-pyrimidyl-5-amidothiophenes has been synthesized and, evaluated for AKT inhibition. SAR studies resulted in potent inhibitors of, AKT with IC(50) values as low as single digit nanomolar as represented by, compound 2aa. Compound 2aa showed cellular activity including, antiproliferation and downstream target modulation. Selectivity profile is, described. A co-crystal of 2aa with PKA is determined and discussed.
About this Structure
2GU8 is a Protein complex structure of sequences from Homo sapiens with as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
Reference
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies., Lin X, Murray JM, Rico AC, Wang MX, Chu DT, Zhou Y, Del Rosario M, Kaufman S, Ma S, Fang E, Crawford K, Jefferson AB, Bioorg Med Chem Lett. 2006 Aug 15;16(16):4163-8. Epub 2006 Jun 9. PMID:16765046
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