View source for 2bge


==Structure-based design of Protein Tyrosine Phosphatase-1B Inhibitors==
<StructureSection load='2bge' size='340' side='right'caption='[[2bge]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[2bge]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BGE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2BGE FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=T2D:1,2,5-THIADIAZOLIDIN-3-ONE-1,1-DIOXIDE'>T2D</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1a5y|1a5y]], [[1aax|1aax]], [[1bzc|1bzc]], [[1bzh|1bzh]], [[1bzj|1bzj]], [[1c83|1c83]], [[1c84|1c84]], [[1c85|1c85]], [[1c86|1c86]], [[1c87|1c87]], [[1c88|1c88]], [[1ecv|1ecv]], [[1een|1een]], [[1eeo|1eeo]], [[1g1f|1g1f]], [[1g1g|1g1g]], [[1g1h|1g1h]], [[1g7f|1g7f]], [[1g7g|1g7g]], [[1gfy|1gfy]], [[1i57|1i57]], [[1jf7|1jf7]], [[1kak|1kak]], [[1kav|1kav]], [[1l8g|1l8g]], [[1lqf|1lqf]], [[1nl9|1nl9]], [[1nny|1nny]], [[1no6|1no6]], [[1nwe|1nwe]], [[1nwl|1nwl]], [[1nz7|1nz7]], [[1oem|1oem]], [[1oeo|1oeo]], [[1oes|1oes]], [[1oet|1oet]], [[1oeu|1oeu]], [[1oev|1oev]], [[1ony|1ony]], [[1onz|1onz]], [[1pa1|1pa1]], [[1ph0|1ph0]], [[1ptt|1ptt]], [[1ptu|1ptu]], [[1ptv|1ptv]], [[1pty|1pty]], [[1pxh|1pxh]], [[1pyn|1pyn]], [[1q1m|1q1m]], [[1q6j|1q6j]], [[1q6m|1q6m]], [[1q6n|1q6n]], [[1q6p|1q6p]], [[1q6s|1q6s]], [[1q6t|1q6t]], [[1qxk|1qxk]], [[1sug|1sug]], [[1t48|1t48]], [[1t49|1t49]], [[1t4j|1t4j]], [[1wax|1wax]], [[1xbo|1xbo]], [[2bgd|2bgd]]</div></td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] </span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2bge FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bge OCA], [https://pdbe.org/2bge PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2bge RCSB], [https://www.ebi.ac.uk/pdbsum/2bge PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2bge 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/bg/2bge_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=2bge ConSurf].
<div style="clear:both"></div>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Using structure-based design, a new class of inhibitors of protein tyrosine phosphatase-1B (PTP1B) has been identified, which incorporate the 1,2,5-thiadiazolidin-3-one-1,1-dioxide template.

Structure-based design of protein tyrosine phosphatase-1B inhibitors.,Black E, Breed J, Breeze AL, Embrey K, Garcia R, Gero TW, Godfrey L, Kenny PW, Morley AD, Minshull CA, Pannifer AD, Read J, Rees A, Russell DJ, Toader D, Tucker J Bioorg Med Chem Lett. 2005 May 16;15(10):2503-7. PMID:15863305<ref>PMID:15863305</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 2bge" style="background-color:#fffaf0;"></div>

==See Also==
*[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Human]]
[[Category: Large Structures]]
[[Category: Protein-tyrosine-phosphatase]]
[[Category: Black, E]]
[[Category: Breed, J]]
[[Category: Breeze, A L]]
[[Category: Embrey, K]]
[[Category: Garcia, R]]
[[Category: Gero, T W]]
[[Category: Godfrey, L]]
[[Category: Kenny, P W]]
[[Category: Minshull, C A]]
[[Category: Morley, A D]]
[[Category: Pannifer, A D]]
[[Category: Read, J]]
[[Category: Rees, A]]
[[Category: Russell, D J]]
[[Category: Toader, D]]
[[Category: Tucker, J]]
[[Category: 1-dioxide template]]
[[Category: 5-thiadiazolidin-3-one-1]]
[[Category: Hydrolase]]
[[Category: Protein tyrosine phosphatase]]