2gu8

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[[Image:2gu8.jpg|left|200px]]
[[Image:2gu8.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2gu8 |SIZE=350|CAPTION= <scene name='initialview01'>2gu8</scene>, resolution 2.20&Aring;
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The line below this paragraph, containing "STRUCTURE_2gu8", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=796:N-[(1S)-2-AMINO-1-(2,4-DICHLOROBENZYL)ETHYL]-5-[2-(METHYLAMINO)PYRIMIDIN-4-YL]THIOPHENE-2-CARBOXAMIDE'>796</scene>, <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_2gu8| PDB=2gu8 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2gu8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2gu8 OCA], [http://www.ebi.ac.uk/pdbsum/2gu8 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2gu8 RCSB]</span>
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}}
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'''Discovery of 2-Pyrimidyl-5-Amidothiophenes as Novel and Potent Inhibitors for AKT: Synthesis and SAR Studies'''
'''Discovery of 2-Pyrimidyl-5-Amidothiophenes as Novel and Potent Inhibitors for AKT: Synthesis and SAR Studies'''
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==About this Structure==
==About this Structure==
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2GU8 is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GU8 OCA].
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Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GU8 OCA].
==Reference==
==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:[http://www.ncbi.nlm.nih.gov/pubmed/16765046 16765046]
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:[http://www.ncbi.nlm.nih.gov/pubmed/16765046 16765046]
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[[Category: Homo sapiens]]
 
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Protein complex]]
 
[[Category: Murray, J M.]]
[[Category: Murray, J M.]]
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[[Category: akt]]
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[[Category: Akt]]
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[[Category: camp-dependent protein kinase]]
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[[Category: Camp-dependent protein kinase]]
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[[Category: drug design]]
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[[Category: Drug design]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: pka]]
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[[Category: Pka]]
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[[Category: ternary complex]]
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[[Category: Ternary complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:32:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:21:42 2008''
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Revision as of 02:32, 4 May 2008

Image:2gu8.jpg

Template:STRUCTURE 2gu8

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

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 Page seeded by OCA on Sun May 4 05:32:46 2008

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