2f70

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[[Image:2f70.png|left|200px]]
 
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{{STRUCTURE_2f70| PDB=2f70 | SCENE= }}
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==Protein tyrosine phosphatase 1B with sulfamic acid inhibitors==
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<StructureSection load='2f70' size='340' side='right'caption='[[2f70]], [[Resolution|resolution]] 2.12&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2f70]] 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=2F70 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2F70 FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.12&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=UN6:(3-{[3-(3-SULFOAMINO-PHENYL)-PROPIONYLAMINO]-METHYL}-PHENYL)-SULFAMIC+ACID'>UN6</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2f70 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2f70 OCA], [https://pdbe.org/2f70 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2f70 RCSB], [https://www.ebi.ac.uk/pdbsum/2f70 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2f70 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/f7/2f70_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</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=2f70 ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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High-throughput screening of the P&amp;GP corporate repository against several protein tyrosine phosphatases identified the sulfamic acid moiety as potential phosphotyrosine mimetic. Incorporation of the sulfamic acid onto a 1,2,3,4-tetrahydroisoquinoline scaffold provided a promising starting point for PTP1B inhibitor design.
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===Protein tyrosine phosphatase 1B with sulfamic acid inhibitors===
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1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors.,Klopfenstein SR, Evdokimov AG, Colson AO, Fairweather NT, Neuman JJ, Maier MB, Gray JL, Gerwe GS, Stake GE, Howard BW, Farmer JA, Pokross ME, Downs TR, Kasibhatla B, Peters KG Bioorg Med Chem Lett. 2006 Mar 15;16(6):1574-8. Epub 2006 Jan 4. PMID:16386905<ref>PMID:16386905</ref>
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{{ABSTRACT_PUBMED_16386905}}
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==About this Structure==
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<div class="pdbe-citations 2f70" style="background-color:#fffaf0;"></div>
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[[2f70]] is a 1 chain structure of [[Proten tyrosine phosphatase]] and [[Tyrosine phosphatase]] with 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=2F70 OCA].
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==See Also==
==See Also==
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*[[Proten tyrosine phosphatase|Proten tyrosine phosphatase]]
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*[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]]
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*[[Tyrosine phosphatase|Tyrosine phosphatase]]
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== References ==
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<references/>
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==Reference==
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__TOC__
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<ref group="xtra">PMID:016386905</ref><references group="xtra"/>
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Protein-tyrosine-phosphatase]]
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[[Category: Large Structures]]
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[[Category: Evdokimov, A G.]]
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[[Category: Evdokimov AG]]
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[[Category: Klopfenstein, S R.]]
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[[Category: Klopfenstein SR]]
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[[Category: Pokross, M E.]]
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[[Category: Pokross ME]]
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[[Category: Hydrolase]]
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[[Category: Phosphatase]]
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[[Category: Ptp1b]]
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[[Category: Sulfamic acid]]
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[[Category: Tetrahydroisoquinoline]]
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[[Category: Tyrosine]]
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Current revision

Protein tyrosine phosphatase 1B with sulfamic acid inhibitors

PDB ID 2f70

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