2oag: Difference between revisions

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[[Image:2oag.~~jpg~~|left|200px]]

[[Image:2oag.png|left|200px]]

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~~'''~~Crystal structure of human dipeptidyl peptidase IV (DPPIV) with pyrrolidine-constrained phenethylamine 29g~~'''~~

===Crystal structure of human dipeptidyl peptidase IV (DPPIV) with pyrrolidine-constrained phenethylamine 29g===

~~==Overview==~~

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~~A novel series of pyrrolidine-constrained phenethylamines were developed as dipeptidyl peptidase IV (DPP4) inhibitors for the treatment of type 2 diabetes.~~ The ~~cyclohexene ring of lead-like screening hit 5 was replaced with a pyrrolidine to enable parallel chemistry~~, ~~and protein co-crystal structural data guided~~ the ~~optimization of N-substituents. Employing this strategy, a >400x improvement in potency over~~ the ~~initial hit was realized in rapid fashion~~. ~~Optimized compounds are potent and selective inhibitors with excellent pharmacokinetic profiles~~. ~~Compound 30 was efficacious in vivo~~, ~~lowering blood glucose in ZDF rats that were allowed to feed freely on a mixed meal~~.

The line below this paragraph, {{ABSTRACT_PUBMED_17276063}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 17276063 is the PubMed ID number.

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==About this Structure==

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[[Category: Inhibitor complex]]

[[Category: Serine-peptidase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sun May 4 10~~:31:21 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 00:52:14 2008''

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-[[Image:2oag.jpg|left|200px]]
+{{Seed}}
+[[Image:2oag.png|left|200px]]
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 {{STRUCTURE_2oag|  PDB=2oag  |  SCENE=  }}
-'''Crystal structure of human dipeptidyl peptidase IV (DPPIV) with pyrrolidine-constrained phenethylamine 29g'''
+===Crystal structure of human dipeptidyl peptidase IV (DPPIV) with pyrrolidine-constrained phenethylamine 29g===
-==Overview==
+<!--
-A novel series of pyrrolidine-constrained phenethylamines were developed as dipeptidyl peptidase IV (DPP4) inhibitors for the treatment of type 2 diabetes. The cyclohexene ring of lead-like screening hit 5 was replaced with a pyrrolidine to enable parallel chemistry, and protein co-crystal structural data guided the optimization of N-substituents. Employing this strategy, a &gt;400x improvement in potency over the initial hit was realized in rapid fashion. Optimized compounds are potent and selective inhibitors with excellent pharmacokinetic profiles. Compound 30 was efficacious in vivo, lowering blood glucose in ZDF rats that were allowed to feed freely on a mixed meal.
+The line below this paragraph, {{ABSTRACT_PUBMED_17276063}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 17276063 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_17276063}}
 ==About this Structure==
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 [[Category: Inhibitor complex]]
 [[Category: Serine-peptidase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 10:31:21 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 00:52:14 2008''