2zm3
From Proteopedia
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[[Category: Tyrosine kinase]] | [[Category: Tyrosine kinase]] | ||
[[Category: Tyrosine-protein kinase]] | [[Category: Tyrosine-protein kinase]] | ||
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Revision as of 12:11, 25 June 2008
Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor
Contents |
Overview
Insulin-like growth factor receptor (IGF-1R) is a growth factor receptor tyrosine kinase that acts as a critical mediator of cell proliferation and survival. This receptor is over-expressed or activated in tumor cells and is emerging as a novel target in cancer therapy. Efforts in our "Hit to Lead" group have generated a novel series of submicromolar IGF-1R inhibitors based on a isoquinolinedione template originating from a Lance enzyme HTS screen. Chemical triage and parallel synthesis incorporating focused library arrays were instrumental in moving these investigations through the Wyeth exploratory medicinal chemistry process. The strategies, synthesis, and SAR behind this interesting kinase scaffold will be described.
Disease
Known disease associated with this structure: Intrauterine and postnatal growth retardation OMIM:[147370]
About this Structure
2ZM3 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment., Mayer SC, Banker AL, Boschelli F, Di L, Johnson M, Kenny CH, Krishnamurthy G, Kutterer K, Moy F, Petusky S, Ravi M, Tkach D, Tsou HR, Xu W, Bioorg Med Chem Lett. 2008 Jun 15;18(12):3641-5. Epub 2008 Apr 25. PMID:18501599
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Categories: Homo sapiens | Receptor protein-tyrosine kinase | Single protein | Boschelli, F. | Dwyer, B. | Johnson, M. | Mayer, S C. | Xu, W. | Atp-binding | Cleavage on pair of basic residue | Disease mutation | Glycoprotein | Igfr | Membrane | Nucleotide-binding | Phosphoprotein | Polymorphism | Protein-inhibitor complex | Receptor | Transferase | Transmembrane | Tyrosine kinase | Tyrosine-protein kinase
