2h4k: Difference between revisions

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[[Image:2h4k.gif|left|200px]]


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==Crystal structure of PTP1B with a monocyclic thiophene inhibitor==
The line below this paragraph, containing "STRUCTURE_2h4k", creates the "Structure Box" on the page.
<StructureSection load='2h4k' size='340' side='right'caption='[[2h4k]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
You may change the PDB parameter (which sets the PDB file loaded into the applet)  
== Structural highlights ==
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
<table><tr><td colspan='2'>[[2h4k]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2H4K OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2H4K FirstGlance]. <br>
or leave the SCENE parameter empty for the default display.
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.3&#8491;</td></tr>
-->
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=509:4-BROMO-3-(CARBOXYMETHOXY)-5-PHENYLTHIOPHENE-2-CARBOXYLIC+ACID'>509</scene></td></tr>
{{STRUCTURE_2h4k| PDB=2h4k |  SCENE= }}
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2h4k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2h4k OCA], [https://pdbe.org/2h4k PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2h4k RCSB], [https://www.ebi.ac.uk/pdbsum/2h4k PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2h4k ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/PTN1_HUMAN PTN1_HUMAN] Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response. Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EIF2AK3/PERK. May play an important role in CKII- and p60c-src-induced signal transduction cascades. May regulate the EFNA5-EPHA3 signaling pathway which modulates cell reorganization and cell-cell repulsion.<ref>PMID:21135139</ref> <ref>PMID:22169477</ref>
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/h4/2h4k_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2h4k ConSurf].
<div style="clear:both"></div>


'''Crystal structure of PTP1B with a monocyclic thiophene inhibitor'''
==See Also==
 
*[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]]
 
== References ==
==Overview==
<references/>
A series of monocyclic thiophenes was designed and synthesized as PTP1B inhibitors. Guided by X-ray co-crystal structural information and computational modeling, rational design led to key interactions with Asp48 and improved inhibitory potency against PTP1B.
__TOC__
 
</StructureSection>
==About this Structure==
2H4K is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2H4K OCA].
 
==Reference==
Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: capturing interactions with Asp48., Wan ZK, Lee J, Xu W, Erbe DV, Joseph-McCarthy D, Follows BC, Zhang YL, Bioorg Med Chem Lett. 2006 Sep 15;16(18):4941-5. Epub 2006 Jun 27. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16806920 16806920]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein-tyrosine-phosphatase]]
[[Category: Large Structures]]
[[Category: Single protein]]
[[Category: Wan Z-K]]
[[Category: Wan, Z K.]]
[[Category: Xu W]]
[[Category: Xu, W.]]
[[Category: Protein-drug complex structure]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 05:51:33 2008''

Latest revision as of 09:31, 14 February 2024

Crystal structure of PTP1B with a monocyclic thiophene inhibitor

2h4k, resolution 2.30Å

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