2oj9

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[[Image:2oj9.gif|left|200px]]
[[Image:2oj9.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2oj9 |SIZE=350|CAPTION= <scene name='initialview01'>2oj9</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2oj9", 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=BMI:3-[5-(1H-IMIDAZOL-1-YL)-7-METHYL-1H-BENZIMIDAZOL-2-YL]-4-[(PYRIDIN-2-YLMETHYL)AMINO]PYRIDIN-2(1H)-ONE'>BMI</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/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= IGF1R ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2oj9| PDB=2oj9 | 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=2oj9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oj9 OCA], [http://www.ebi.ac.uk/pdbsum/2oj9 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oj9 RCSB]</span>
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}}
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'''Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor'''
'''Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor'''
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[[Category: Jacobson, B L.]]
[[Category: Jacobson, B L.]]
[[Category: Sack, J S.]]
[[Category: Sack, J S.]]
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[[Category: hormone/growth factor]]
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[[Category: Hormone/growth factor]]
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[[Category: igf-1r]]
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[[Category: Igf-1r]]
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[[Category: kinase domain]]
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[[Category: Kinase domain]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:01:57 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:18:39 2008''
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Revision as of 08:01, 4 May 2008

Image:2oj9.gif

Template:STRUCTURE 2oj9

Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor


Contents

Overview

The discovery and synthesis of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor 1-receptor (IGF-1R) are presented. Installing amine containing side chains at the 4-position of pyridone ring significantly improved the enzyme potency. SAR and biological activity of these compounds is presented.

Disease

Known disease associated with this structure: Intrauterine and postnatal growth retardation OMIM:[147370]

About this Structure

2OJ9 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R)., Velaparthi U, Wittman M, Liu P, Stoffan K, Zimmermann K, Sang X, Carboni J, Li A, Attar R, Gottardis M, Greer A, Chang CY, Jacobsen BL, Sack JS, Sun Y, Langley DR, Balasubramanian B, Vyas D, Bioorg Med Chem Lett. 2007 Apr 15;17(8):2317-21. Epub 2007 Feb 4. PMID:17317169 Page seeded by OCA on Sun May 4 11:01:57 2008

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OCA

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