2ghg

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[[Image:2ghg.gif|left|200px]]
[[Image:2ghg.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2ghg |SIZE=350|CAPTION= <scene name='initialview01'>2ghg</scene>, resolution 3.50&Aring;
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The line below this paragraph, containing "STRUCTURE_2ghg", 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=A53:5-{5-[(S)-2-AMINO-3-(1H-INDOL-3-YL)-PROPOXYL]-PYRIDIN-3-YL}-3-[1-(1H-PYRROL-2-YL)-METH-(Z)-YLIDENE]-1,3-DIHYDRO-INDOL-2-ONE'>A53</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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-->
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|DOMAIN=
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{{STRUCTURE_2ghg| PDB=2ghg | SCENE= }}
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|RELATEDENTRY=[[2ayp|2AYP]], [[2fga|2FGA]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ghg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ghg OCA], [http://www.ebi.ac.uk/pdbsum/2ghg PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ghg RCSB]</span>
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}}
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'''h-CHK1 complexed with A431994'''
'''h-CHK1 complexed with A431994'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Park, C.]]
[[Category: Park, C.]]
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[[Category: protein-inhibitor complex]]
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[[Category: Protein-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:06:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:16:44 2008''
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Revision as of 02:06, 4 May 2008

Image:2ghg.gif

Template:STRUCTURE 2ghg

h-CHK1 complexed with A431994


Overview

We describe a series of potent and selective oxindole-pyridine-based protein kinase B/Akt inhibitors. The most potent compound 11n in this series demonstrated an IC(50) of 0.17nM against Akt1 and more than 100-fold selectivity over other Akt isozymes. The selectivity against other protein kinases was highly dependent on the C-3 substitutions at the oxindole scaffold, with unsubstituted 9e or 3-furan-2-ylmethylene (11n) more selective and 3-(1H-pyrrol-2-yl)methylene (11f) or 3-(1H-imidazol-2-yl)methylene (11k) less selective. In a mouse xenograft model, 9d, 11f, and 11n inhibited tumor growth but with accompanying toxicity.

About this Structure

2GHG is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers., Zhu GD, Gandhi VB, Gong J, Luo Y, Liu X, Shi Y, Guan R, Magnone SR, Klinghofer V, Johnson EF, Bouska J, Shoemaker A, Oleksijew A, Jarvis K, Park C, Jong RD, Oltersdorf T, Li Q, Rosenberg SH, Giranda VL, Bioorg Med Chem Lett. 2006 Jul 1;16(13):3424-9. Epub 2006 Apr 27. PMID:16644221 Page seeded by OCA on Sun May 4 05:06:46 2008

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OCA

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