1x70

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:1x70.gif|left|200px]]
+
{{Seed}}
 +
[[Image:1x70.png|left|200px]]
<!--
<!--
Line 9: Line 10:
{{STRUCTURE_1x70| PDB=1x70 | SCENE= }}
{{STRUCTURE_1x70| PDB=1x70 | SCENE= }}
-
'''HUMAN DIPEPTIDYL PEPTIDASE IV IN COMPLEX WITH A BETA AMINO ACID INHIBITOR'''
+
===HUMAN DIPEPTIDYL PEPTIDASE IV IN COMPLEX WITH A BETA AMINO ACID INHIBITOR===
-
==Overview==
+
<!--
-
A novel series of beta-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes. (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin -7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine (1) is a potent, orally active DPP-IV inhibitor (IC(50) = 18 nM) with excellent selectivity over other proline-selective peptidases, oral bioavailability in preclinical species, and in vivo efficacy in animal models. MK-0431, the phosphate salt of compound 1, was selected for development as a potential new treatment for type 2 diabetes.
+
The line below this paragraph, {{ABSTRACT_PUBMED_15634008}}, adds the Publication Abstract to the page
 +
(as it appears on PubMed at http://www.pubmed.gov), where 15634008 is the PubMed ID number.
 +
-->
 +
{{ABSTRACT_PUBMED_15634008}}
==About this Structure==
==About this Structure==
Line 35: Line 39:
[[Category: Beta-propeller]]
[[Category: Beta-propeller]]
[[Category: Dimer]]
[[Category: Dimer]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:38:55 2008''
+
 
 +
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 12:47:16 2008''

Revision as of 09:47, 27 July 2008

Image:1x70.png


PDB ID 1x70

Drag the structure with the mouse to rotate
1x70, resolution 2.10Å ()
Ligands: , , ,
Gene: DPP4, ADCP2, CD26 (Homo sapiens)
Activity: Dipeptidyl-peptidase IV, with EC number 3.4.14.5
Resources: FirstGlance, OCA, RCSB, PDBsum
Coordinates: save as pdb, mmCIF, xml



HUMAN DIPEPTIDYL PEPTIDASE IV IN COMPLEX WITH A BETA AMINO ACID INHIBITOR

Template:ABSTRACT PUBMED 15634008

About this Structure

1X70 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin -7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes., Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, Hickey GJ, Kowalchick JE, Leiting B, Lyons K, Marsilio F, McCann ME, Patel RA, Petrov A, Scapin G, Patel SB, Roy RS, Wu JK, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE, J Med Chem. 2005 Jan 13;48(1):141-51. PMID:15634008

Page seeded by OCA on Sun Jul 27 12:47:16 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1x70"
Personal tools