2zm3

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==Overview==
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{{ABSTRACT_18501599}}
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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.
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==Disease==
==Disease==
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==About this Structure==
==About this Structure==
2ZM3 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2ZM3 OCA].
2ZM3 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2ZM3 OCA].
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==Reference==
 
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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:[http://www.ncbi.nlm.nih.gov/pubmed/18501599 18501599]
 
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Receptor protein-tyrosine kinase]]
[[Category: Receptor protein-tyrosine kinase]]
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[[Category: Tyrosine-protein kinase]]
[[Category: Tyrosine-protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 25 15:11:11 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 25 18:42:59 2008''

Revision as of 15:43, 25 June 2008

Image:2zm3.png

Template:STRUCTURE 2zm3

Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor


Template:ABSTRACT 18501599

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.

Page seeded by OCA on Wed Jun 25 18:42:59 2008

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OCA

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