2zm3: Difference between revisions

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~~==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==

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==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].

~~==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:[http://www.ncbi.nlm.nih.gov/pubmed/18501599 18501599]

[[Category: Homo sapiens]]

[[Category: Receptor protein-tyrosine kinase]]

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[[Category: Tyrosine-protein kinase]]

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@@ Line 12: / Line 12: @@
-==Overview==
+{{ABSTRACT_18501599}}
-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==
@@ Line 20: / Line 19: @@
 ==About this Structure==
 ZM3 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].
-==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:[http://www.ncbi.nlm.nih.gov/pubmed/18501599 18501599]
 [[Category: Homo sapiens]]
 [[Category: Receptor protein-tyrosine kinase]]
@@ Line 47: / Line 43: @@
 [[Category: Tyrosine-protein kinase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 25 15:11:11 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 25 18:42:59 2008''