2qt9

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:2qt9.jpg|left|200px]]
[[Image:2qt9.jpg|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 2qt9 |SIZE=350|CAPTION= <scene name='initialview01'>2qt9</scene>, resolution 2.100&Aring;
+
The line below this paragraph, containing "STRUCTURE_2qt9", creates the "Structure Box" on the page.
-
|SITE=
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=524:(2S,3S)-3-AMINO-4-[(3S)-3-FLUOROPYRROLIDIN-1-YL]-N,N-DIMETHYL-4-OXO-2-(TRANS-4-[1,2,4]TRIAZOLO[1,5-A]PYRIDIN-5-YLCYCLOHEXYL)BUTANAMIDE'>524</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=NDG:2-(ACETYLAMINO)-2-DEOXY-A-D-GLUCOPYRANOSE'>NDG</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Dipeptidyl-peptidase_IV Dipeptidyl-peptidase IV], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5] </span>
+
or leave the SCENE parameter empty for the default display.
-
|GENE= DPP4, ADCP2, CD26 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+
-->
-
|DOMAIN=
+
{{STRUCTURE_2qt9| PDB=2qt9 | SCENE= }}
-
|RELATEDENTRY=[[2qtb|2QTB]]
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2qt9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2qt9 OCA], [http://www.ebi.ac.uk/pdbsum/2qt9 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2qt9 RCSB]</span>
+
-
}}
+
'''Human dipeptidyl peptidase iv/cd26 in complex with a 4-aryl cyclohexylalanine inhibitor'''
'''Human dipeptidyl peptidase iv/cd26 in complex with a 4-aryl cyclohexylalanine inhibitor'''
Line 27: Line 24:
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Scapin, G.]]
[[Category: Scapin, G.]]
-
[[Category: alpha/beta]]
+
[[Category: Alpha/beta]]
-
[[Category: aminopeptidase]]
+
[[Category: Aminopeptidase]]
-
[[Category: beta-propeller]]
+
[[Category: Beta-propeller]]
-
[[Category: dimer]]
+
[[Category: Dimer]]
-
[[Category: glycoprotein]]
+
[[Category: Glycoprotein]]
-
[[Category: hydrolase]]
+
[[Category: Hydrolase]]
-
[[Category: membrane]]
+
[[Category: Membrane]]
-
[[Category: protease]]
+
[[Category: Protease]]
-
[[Category: secreted]]
+
[[Category: Secreted]]
-
[[Category: serine protease]]
+
[[Category: Serine protease]]
-
[[Category: signal-anchor]]
+
[[Category: Signal-anchor]]
-
[[Category: transmembrane]]
+
[[Category: Transmembrane]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 15:38:26 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:53:04 2008''
+

Revision as of 12:38, 4 May 2008

Image:2qt9.jpg

Template:STRUCTURE 2qt9

Human dipeptidyl peptidase iv/cd26 in complex with a 4-aryl cyclohexylalanine inhibitor


Overview

A novel series of 4-arylcyclohexylalanine DPP-4 inhibitors was synthesized and tested for inhibitory activity as well as selectivity over the related proline-specific enzymes DPP-8 and DPP-9. Optimization of this series led to 28 (DPP-4 IC(50)=4.8 nM), which showed an excellent pharmacokinetic profile across several preclinical species. Evaluation of 28 in an oral glucose tolerance test demonstrated that this compound effectively reduced glucose excursion in lean mice.

About this Structure

2QT9 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV., Kaelin DE, Smenton AL, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Duffy JL, Bioorg Med Chem Lett. 2007 Nov 1;17(21):5806-11. Epub 2007 Aug 26. PMID:17851076 Page seeded by OCA on Sun May 4 15:38:26 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2qt9"
Personal tools