1onz

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:1onz.gif|left|200px]]
[[Image:1onz.gif|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 1onz |SIZE=350|CAPTION= <scene name='initialview01'>1onz</scene>, resolution 2.40&Aring;
+
The line below this paragraph, containing "STRUCTURE_1onz", 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=968:2-[(7-HYDROXY-NAPHTHALEN-1-YL)-OXALYL-AMINO]-BENZOIC+ACID'>968</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/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] </span>
+
or leave the SCENE parameter empty for the default display.
-
|GENE= PTPN1 OR PTP1B ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+
-->
-
|DOMAIN=
+
{{STRUCTURE_1onz| PDB=1onz | SCENE= }}
-
|RELATEDENTRY=[[1nl9|1NL9]], [[1nny|1NNY]], [[1no6|1No6]], [[1nz7|1NZ7]], [[1ony|1ONY]]
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1onz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1onz OCA], [http://www.ebi.ac.uk/pdbsum/1onz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1onz RCSB]</span>
+
-
}}
+
'''Oxalyl-aryl-Amino Benzoic acid Inhibitors of PTP1B, compound 8b'''
'''Oxalyl-aryl-Amino Benzoic acid Inhibitors of PTP1B, compound 8b'''
Line 43: Line 40:
[[Category: Xin, Z.]]
[[Category: Xin, Z.]]
[[Category: Zinker, B A.]]
[[Category: Zinker, B A.]]
-
[[Category: oxalyl-aryl-benzoic acid compound with napthyl moiety anchor inhibitor]]
+
[[Category: Oxalyl-aryl-benzoic acid compound with napthyl moiety anchor inhibitor]]
-
[[Category: protein tyrosine phosphatase]]
+
[[Category: Protein tyrosine phosphatase]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:05:09 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:47:58 2008''
+

Revision as of 01:05, 3 May 2008

Image:1onz.gif

Template:STRUCTURE 1onz

Oxalyl-aryl-Amino Benzoic acid Inhibitors of PTP1B, compound 8b


Overview

Protein Tyrosine phosphatase 1B (PTP1B) has been implicated as a key negative regulator of both insulin and leptin signaling pathways. Using an NMR-based screening approach with 15N- and 13C-labeled PTP1B, we have identified 2,3-dimethylphenyloxalylaminobenzoic acid (1) as a general, reversible, and competitive PTPase inhibitor. Structure-based approach guided by X-ray crystallography facilitated the development of 1 into a novel series of potent and selective PTP1B inhibitors occupying both the catalytic site and a portion of the noncatalytic, second phosphotyrosine binding site. Interestingly, oral biovailability has been observed in rats for some compounds. Furthermore, we demonstrated in vivo plasma glucose lowering effects with compound 12d in ob/ob mice.

About this Structure

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

Reference

Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B., Liu G, Szczepankiewicz BG, Pei Z, Janowick DA, Xin Z, Hajduk PJ, Abad-Zapatero C, Liang H, Hutchins CW, Fesik SW, Ballaron SJ, Stashko MA, Lubben T, Mika AK, Zinker BA, Trevillyan JM, Jirousek MR, J Med Chem. 2003 May 22;46(11):2093-103. PMID:12747781 Page seeded by OCA on Sat May 3 04:05:09 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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