2g5p: Difference between revisions

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[[Image:2g5p.~~gif~~|left|200px]]

[[Image:2g5p.png|left|200px]]

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~~'''~~Crystal structure of human dipeptidyl peptidase IV (DPPIV) complexed with cyanopyrrolidine (C5-pro-pro) inhibitor 21ac~~'''~~

===Crystal structure of human dipeptidyl peptidase IV (DPPIV) complexed with cyanopyrrolidine (C5-pro-pro) inhibitor 21ac===

~~==Overview==~~

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~~A series of (5~~-~~substituted pyrrolidinyl~~-2-carbonyl)-2-cyanopyrrolidine (C5-Pro-Pro) analogues was discovered as dipeptidyl peptidase IV (DPPIV) inhibitors as a potential treatment of diabetes and obesity. X-ray crystallography data show that these inhibitors bind to the catalytic site of DPPIV with the cyano group forming a covalent bond with the serine residue of DPPIV. The ~~C5-substituents make various interactions with the enzyme and affect potency~~, ~~chemical stability~~, ~~selectivity, and PK properties of~~ the ~~inhibitors~~. ~~Optimized analogues are extremely potent with subnanomolar K(i~~)'s, ~~are chemically stable, show very little potency decrease in~~ the ~~presence of plasma, and exhibit more than 1,000~~-~~fold selectivity against related peptidases. The best compounds also possess good PK and are efficacious in lowering blood glucose in an oral glucose tolerance test in ZDF rats.~~

The line below this paragraph, {{ABSTRACT_PUBMED_16759095}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 16759095 is the PubMed ID number.

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==About this Structure==

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[[Category: Beta-propeller]]

[[Category: Serine peptidase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sun May 4 04~~:43:06 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:44:34 2008''

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@@ Line 1: / Line 1: @@
-[[Image:2g5p.gif|left|200px]]
+{{Seed}}
+[[Image:2g5p.png|left|200px]]
 <!--
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 {{STRUCTURE_2g5p|  PDB=2g5p  |  SCENE=  }}
-'''Crystal structure of human dipeptidyl peptidase IV (DPPIV) complexed with cyanopyrrolidine (C5-pro-pro) inhibitor 21ac'''
+===Crystal structure of human dipeptidyl peptidase IV (DPPIV) complexed with cyanopyrrolidine (C5-pro-pro) inhibitor 21ac===
-==Overview==
+<!--
-A series of (5-substituted pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidine (C5-Pro-Pro) analogues was discovered as dipeptidyl peptidase IV (DPPIV) inhibitors as a potential treatment of diabetes and obesity. X-ray crystallography data show that these inhibitors bind to the catalytic site of DPPIV with the cyano group forming a covalent bond with the serine residue of DPPIV. The C5-substituents make various interactions with the enzyme and affect potency, chemical stability, selectivity, and PK properties of the inhibitors. Optimized analogues are extremely potent with subnanomolar K(i)'s, are chemically stable, show very little potency decrease in the presence of plasma, and exhibit more than 1,000-fold selectivity against related peptidases. The best compounds also possess good PK and are efficacious in lowering blood glucose in an oral glucose tolerance test in ZDF rats.
+The line below this paragraph, {{ABSTRACT_PUBMED_16759095}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 16759095 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_16759095}}
 ==About this Structure==
@@ Line 31: / Line 35: @@
 [[Category: Beta-propeller]]
 [[Category: Serine peptidase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 04:43:06 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:44:34 2008''