5kqm: Difference between revisions

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'''Unreleased structure'''


The entry 5kqm is ON HOLD  until Paper Publication
==Co-crystal structure of LMW-PTP in complex with MES==
<StructureSection load='5kqm' size='340' side='right' caption='[[5kqm]], [[Resolution|resolution]] 1.91&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5kqm]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KQM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5KQM FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5kqg|5kqg]], [[5kql|5kql]], [[5kqp|5kqp]]</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=5kqm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kqm OCA], [http://pdbe.org/5kqm PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5kqm RCSB], [http://www.ebi.ac.uk/pdbsum/5kqm PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5kqm ProSAT]</span></td></tr>
</table>
== Function ==
[[http://www.uniprot.org/uniprot/PPAC_HUMAN PPAC_HUMAN]] Acts on tyrosine phosphorylated proteins, low-MW aryl phosphates and natural and synthetic acyl phosphates. Isoform 3 does not possess phosphatase activity.
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The low molecular weight protein tyrosine phosphatase (LMW-PTP) is a regulator of a number of signaling pathways and has been implicated as a potential target for oncology and diabetes/obesity. There is significant therapeutic interest in developing potent and selective inhibitors to control LMW-PTP activity. We report the discovery of a novel class of LMW-PTP inhibitors derived from sulfophenyl acetic amide (SPAA), some of which exhibit greater than 50-fold preference for LMW-PTP over a large panel of PTPs. X-ray crystallography reveals that binding of SPAA-based inhibitors induces a striking conformational change in the LMW-PTP active site, leading to the formation of a previously undisclosed hydrophobic pocket to accommodate the alpha-phenyl ring in the ligand. This induced-fit mechanism is likely a major contributor responsible for the exquisite inhibitor selectivity.


Authors: Wang, J., Zhang, Z.-Y., Yu, Z.-H.
Inhibition of Low Molecular Weight Protein Tyrosine Phosphatase by an Induced-Fit Mechanism.,He R, Wang J, Yu ZH, Zhang RY, Liu S, Wu L, Zhang ZY J Med Chem. 2016 Oct 3. PMID:27676368<ref>PMID:27676368</ref>


Description: Co-crystal structure of LMW-PTP in complex with MES
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
[[Category: Unreleased Structures]]
</div>
[[Category: Yu, Z.-H]]
<div class="pdbe-citations 5kqm" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Wang, J]]
[[Category: Wang, J]]
[[Category: Zhang, Z.-Y]]
[[Category: Yu, Z H]]
[[Category: Zhang, Z Y]]
[[Category: Complex]]
[[Category: Hydrolase]]
[[Category: Inhibitor]]
[[Category: Lmw-ptp]]
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