5vf6: Difference between revisions
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==Crystal structure of single chain variable fragment (scFv45).== | |||
<StructureSection load='5vf6' size='340' side='right' caption='[[5vf6]], [[Resolution|resolution]] 1.64Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[5vf6]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5VF6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5VF6 FirstGlance]. <br> | |||
</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5vf6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5vf6 OCA], [http://pdbe.org/5vf6 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5vf6 RCSB], [http://www.ebi.ac.uk/pdbsum/5vf6 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5vf6 ProSAT]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
The protein tyrosine phosphatase PTP1B is a major regulator of glucose homeostasis and energy metabolism, and a validated target for therapeutic intervention in diabetes and obesity. Nevertheless, it is a challenging target for inhibitor development. Previously, we generated a recombinant antibody (scFv45) that recognizes selectively the oxidized, inactive conformation of PTP1B. Here, we provide a molecular basis for its interaction with reversibly oxidized PTP1B. Furthermore, we have identified a small molecule inhibitor that mimics the effects of scFv45. Our data provide proof-of-concept that stabilization of PTP1B in an inactive, oxidized conformation by small molecules can promote insulin and leptin signaling. This work illustrates a novel paradigm for inhibiting the signaling function of PTP1B that may be exploited for therapeutic intervention in diabetes and obesity. | |||
Harnessing insulin- and leptin-induced oxidation of PTP1B for therapeutic development.,Krishnan N, Bonham CA, Rus IA, Shrestha OK, Gauss CM, Haque A, Tocilj A, Joshua-Tor L, Tonks NK Nat Commun. 2018 Jan 18;9(1):283. doi: 10.1038/s41467-017-02252-2. PMID:29348454<ref>PMID:29348454</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
<div class="pdbe-citations 5vf6" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Joshua-Tor, L]] | |||
[[Category: Shrestha, O K]] | |||
[[Category: Tocilj, A]] | |||
[[Category: Tonks, N K]] | |||
[[Category: Conformation-sensor antibody]] | |||
[[Category: Immune system]] | |||
[[Category: Intrabody]] | |||
[[Category: Scfv]] | |||
[[Category: Single chain variable fragment]] | |||
Revision as of 05:51, 31 January 2018
Crystal structure of single chain variable fragment (scFv45).
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