2fjm

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{{Seed}}
 
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[[Image:2fjm.png|left|200px]]
 
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==The structure of phosphotyrosine phosphatase 1B in complex with compound 2==
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The line below this paragraph, containing "STRUCTURE_2fjm", creates the "Structure Box" on the page.
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<StructureSection load='2fjm' size='340' side='right'caption='[[2fjm]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[2fjm]] is a 2 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=2FJM OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2FJM FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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]] 2.1&#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=073:(4-{(2S,4E)-2-(1H-1,2,3-BENZOTRIAZOL-1-YL)-2-[4-(METHOXYCARBONYL)PHENYL]-5-PHENYLPENT-4-ENYL}PHENYL)(DIFLUORO)METHYLPHOSPHONIC+ACID'>073</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
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{{STRUCTURE_2fjm| PDB=2fjm | SCENE= }}
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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=2fjm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2fjm OCA], [https://pdbe.org/2fjm PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2fjm RCSB], [https://www.ebi.ac.uk/pdbsum/2fjm PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2fjm 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/fj/2fjm_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=2fjm 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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PTP-1B represents an attractive target for the treatment of type 2 diabetes and obesity. Given the role that protein phosphatases play in the regulation of many biologically relevant processes, inhibitors against PTP-1B must be not only potent, but also selective. It has been extremely difficult to synthesize inhibitors that are selective over the highly homologous TCPTP. We have successfully exploited the conservative Leu119 to Val substitution between the two enzymes to synthesize a PTP-1B inhibitor that is an order of magnitude more selective over TCPTP. Structural analyses of PTP-1B/inhibitor complexes show a conformation-assisted inhibition mechanism as the basis for selectivity. Such an inhibitory mechanism may be applicable to other homologous enzymes.
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===The structure of phosphotyrosine phosphatase 1B in complex with compound 2===
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Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase.,Asante-Appiah E, Patel S, Desponts C, Taylor JM, Lau C, Dufresne C, Therien M, Friesen R, Becker JW, Leblanc Y, Kennedy BP, Scapin G J Biol Chem. 2006 Mar 24;281(12):8010-5. Epub 2006 Jan 6. PMID:16407290<ref>PMID:16407290</ref>
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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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<div class="pdbe-citations 2fjm" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_16407290}}, adds the Publication Abstract to the page
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*[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 16407290 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_16407290}}
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__TOC__
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</StructureSection>
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==About this Structure==
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2FJM is a 2 chains structure of sequences 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=2FJM OCA].
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==Reference==
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Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase., Asante-Appiah E, Patel S, Desponts C, Taylor JM, Lau C, Dufresne C, Therien M, Friesen R, Becker JW, Leblanc Y, Kennedy BP, Scapin G, J Biol Chem. 2006 Mar 24;281(12):8010-5. Epub 2006 Jan 6. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16407290 16407290]
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[[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: Asante-Appiah, E.]]
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[[Category: Asante-Appiah E]]
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[[Category: Becker, J W.]]
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[[Category: Becker JW]]
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[[Category: Desponts, C.]]
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[[Category: Desponts C]]
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[[Category: Dufresne, C.]]
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[[Category: Dufresne C]]
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[[Category: Friesen, R.]]
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[[Category: Friesen R]]
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[[Category: Lau, C.]]
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[[Category: Lau C]]
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[[Category: Leblanc, Y.]]
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[[Category: Leblanc Y]]
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[[Category: Patel, S.]]
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[[Category: Patel S]]
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[[Category: Scapin, G.]]
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[[Category: Scapin G]]
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[[Category: Taylor, J M.]]
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[[Category: Taylor JM]]
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[[Category: Therien, M.]]
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[[Category: Therien M]]
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[[Category: Hydrolase]]
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[[Category: Phosphatase]]
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[[Category: Secondary binding site]]
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[[Category: Selectivity]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Dec 17 13:07:28 2008''
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Current revision

The structure of phosphotyrosine phosphatase 1B in complex with compound 2

PDB ID 2fjm

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