This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


1nl9

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:1nl9.jpg|left|200px]]
+
{{Seed}}
 +
[[Image:1nl9.png|left|200px]]
<!--
<!--
Line 9: Line 10:
{{STRUCTURE_1nl9| PDB=1nl9 | SCENE= }}
{{STRUCTURE_1nl9| PDB=1nl9 | SCENE= }}
-
'''Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Compound 12 Using a Linked-Fragment Strategy'''
+
===Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Compound 12 Using a Linked-Fragment Strategy===
-
==Overview==
+
<!--
-
Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that downregulates the insulin receptor. Inhibition of PTP1B is expected to improve insulin action, and the design of small molecule PTP1B inhibitors to treat type II diabetes has received considerable attention. In this work, NMR-based screening identified a nonselective competitive inhibitor of PTP1B. A second site ligand was also identified by NMR-based screening and then linked to the catalytic site ligand by rational design. X-ray data confirmed that the inhibitor bound with the catalytic site in the native, "open" conformation. The final compound displayed excellent potency and good selectivity over many other phosphatases. The modular approach to drug design described in this work should be applicable for the design of potent and selective inhibitors of other therapeutically relevant protein tyrosine phosphatases.
+
The line below this paragraph, {{ABSTRACT_PUBMED_12670229}}, adds the Publication Abstract to the page
 +
(as it appears on PubMed at http://www.pubmed.gov), where 12670229 is the PubMed ID number.
 +
-->
 +
{{ABSTRACT_PUBMED_12670229}}
==About this Structure==
==About this Structure==
Line 40: Line 44:
[[Category: Dual-site oxamic acid inhibitor bound to p-loop]]
[[Category: Dual-site oxamic acid inhibitor bound to p-loop]]
[[Category: Protein tyrosine phosphatase fold]]
[[Category: Protein tyrosine phosphatase fold]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 02:40:01 2008''
+
 
 +
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 14:38:30 2008''

Revision as of 11:38, 27 July 2008

Image:1nl9.png

Template:STRUCTURE 1nl9

Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Compound 12 Using a Linked-Fragment Strategy

Template:ABSTRACT PUBMED 12670229

About this Structure

1NL9 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy., Szczepankiewicz BG, Liu G, Hajduk PJ, Abad-Zapatero C, Pei Z, Xin Z, Lubben TH, Trevillyan JM, Stashko MA, Ballaron SJ, Liang H, Huang F, Hutchins CW, Fesik SW, Jirousek MR, J Am Chem Soc. 2003 Apr 9;125(14):4087-96. PMID:12670229

Page seeded by OCA on Sun Jul 27 14:38:30 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1nl9"
Personal tools