2oj9
From Proteopedia
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==Overview== | ==Overview== | ||
| - | The discovery and synthesis of | + | 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== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Transferase]] | [[Category: Transferase]] | ||
| - | [[Category: Jacobson, B | + | [[Category: Jacobson, B L.]] |
| - | [[Category: Sack, J | + | [[Category: Sack, J S.]] |
[[Category: BMI]] | [[Category: BMI]] | ||
[[Category: hormone/growth factor]] | [[Category: hormone/growth factor]] | ||
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[[Category: kinase domain]] | [[Category: kinase domain]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:19:07 2008'' |
Revision as of 16:19, 21 February 2008
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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 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 Thu Feb 21 18:19:07 2008
