1t4j: Difference between revisions

From Proteopedia
Jump to navigationJump to search
← Older editNewer edit →
OCA (talk | contribs)
Bots, Bureaucrats, journal, Administrators
3,331,613 edits
No edit summary
OCA (talk | contribs)
Bots, Bureaucrats, journal, Administrators
3,331,613 edits
No edit summary
Line 1: Line 1:
[[Image:1t4j.jpg|left|200px]]
{{Seed}}
[[Image:1t4j.png|left|200px]]


<!--
<!--
Line 9: Line 10:
{{STRUCTURE_1t4j|  PDB=1t4j  |  SCENE=  }}  
{{STRUCTURE_1t4j|  PDB=1t4j  |  SCENE=  }}  


'''Allosteric Inhibition of Protein Tyrosine Phosphatase 1B'''
===Allosteric Inhibition of Protein Tyrosine Phosphatase 1B===




==Overview==
<!--
Obesity and type II diabetes are closely linked metabolic syndromes that afflict &gt;100 million people worldwide. Although protein tyrosine phosphatase 1B (PTP1B) has emerged as a promising target for the treatment of both syndromes, the discovery of pharmaceutically acceptable inhibitors that bind at the active site remains a substantial challenge. Here we describe the discovery of an allosteric site in PTP1B. Crystal structures of PTP1B in complex with allosteric inhibitors reveal a novel site located approximately 20 A from the catalytic site. We show that allosteric inhibitors prevent formation of the active form of the enzyme by blocking mobility of the catalytic loop, thereby exploiting a general mechanism used by tyrosine phosphatases. Notably, these inhibitors exhibit selectivity for PTP1B and enhance insulin signaling in cells. Allosteric inhibition is a promising strategy for targeting PTP1B and constitutes a mechanism that may be applicable to other tyrosine phosphatases.
The line below this paragraph, {{ABSTRACT_PUBMED_15258570}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 15258570 is the PubMed ID number.
-->
{{ABSTRACT_PUBMED_15258570}}


==About this Structure==
==About this Structure==
Line 35: Line 39:
[[Category: Zhu, J.]]
[[Category: Zhu, J.]]
[[Category: Allosteric inhibition protein tyrosine phosphatase 1b]]
[[Category: Allosteric inhibition protein tyrosine phosphatase 1b]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 09:31:11 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 09:37:42 2008''
Retrieved from "https://proteopedia.org/1t4j"