2oj9
From Proteopedia
(New page: 200px<br /> <applet load="2oj9" size="450" color="white" frame="true" align="right" spinBox="true" caption="2oj9, resolution 2.00Å" /> '''Structure of IGF-1R...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:2oj9.gif|left|200px]]<br /> | + | [[Image:2oj9.gif|left|200px]]<br /><applet load="2oj9" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2oj9" size=" | + | |
caption="2oj9, resolution 2.00Å" /> | caption="2oj9, resolution 2.00Å" /> | ||
'''Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor'''<br /> | '''Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor'''<br /> | ||
| Line 6: | Line 5: | ||
==Overview== | ==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. | 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:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=147370 147370]] | ||
==About this Structure== | ==About this Structure== | ||
| - | 2OJ9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with BMI as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http:// | + | 2OJ9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=BMI:'>BMI</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OJ9 OCA]. |
==Reference== | ==Reference== | ||
| Line 25: | Line 21: | ||
[[Category: kinase domain]] | [[Category: kinase domain]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 15:28:23 2008'' |
Revision as of 13:28, 23 January 2008
|
Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor
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.
About this Structure
2OJ9 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 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 Wed Jan 23 15:28:23 2008
