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2bge

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Revision as of 06:42, 16 May 2018

Structure-based design of Protein Tyrosine Phosphatase-1B Inhibitors

Structural highlights

2bge is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Related:	1a5y, 1aax, 1bzc, 1bzh, 1bzj, 1c83, 1c84, 1c85, 1c86, 1c87, 1c88, 1ecv, 1een, 1eeo, 1g1f, 1g1g, 1g1h, 1g7f, 1g7g, 1gfy, 1i57, 1jf7, 1kak, 1kav, 1l8g, 1lqf, 1nl9, 1nny, 1no6, 1nwe, 1nwl, 1nz7, 1oem, 1oeo, 1oes, 1oet, 1oeu, 1oev, 1ony, 1onz, 1pa1, 1ph0, 1ptt, 1ptu, 1ptv, 1pty, 1pxh, 1pyn, 1q1m, 1q6j, 1q6m, 1q6n, 1q6p, 1q6s, 1q6t, 1qxk, 1sug, 1t48, 1t49, 1t4j, 1wax, 1xbo, 2bgd
Activity:	Protein-tyrosine-phosphatase, with EC number 3.1.3.48
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[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.^[1] ^[2]

Evolutionary Conservation

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

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^[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Nievergall E, Janes PW, Stegmayer C, Vail ME, Haj FG, Teng SW, Neel BG, Bastiaens PI, Lackmann M. PTP1B regulates Eph receptor function and trafficking. J Cell Biol. 2010 Dec 13;191(6):1189-203. doi: 10.1083/jcb.201005035. Epub 2010, Dec 6. PMID:21135139 doi:10.1083/jcb.201005035
↑ Krishnan N, Fu C, Pappin DJ, Tonks NK. H2S-Induced sulfhydration of the phosphatase PTP1B and its role in the endoplasmic reticulum stress response. Sci Signal. 2011 Dec 13;4(203):ra86. doi: 10.1126/scisignal.2002329. PMID:22169477 doi:10.1126/scisignal.2002329
↑ 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. Structure-based design of protein tyrosine phosphatase-1B inhibitors. Bioorg Med Chem Lett. 2005 May 16;15(10):2503-7. PMID:15863305 doi:http://dx.doi.org/10.1016/j.bmcl.2005.03.068

1 Structural highlights
2 Function
3 Evolutionary Conservation
4 Publication Abstract from PubMed
5 See Also
6 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2bge"

@@ Line 1: / Line 1: @@
 ==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. 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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2BGE FirstGlance]. <br>
+<table><tr><td colspan='2'>[[2bge]] is a 1 chain structure with sequence from [http://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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2BGE FirstGlance]. <br>
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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">[[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]]</td></tr>
 <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://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'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2bge FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bge OCA], [http://pdbe.org/2bge PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2bge RCSB], [http://www.ebi.ac.uk/pdbsum/2bge PDBsum]</span></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=2bge FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bge OCA], [http://pdbe.org/2bge PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2bge RCSB], [http://www.ebi.ac.uk/pdbsum/2bge PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2bge ProSAT]</span></td></tr>
 </table>
 == Function ==
@@ Line 14: / Line 15: @@
 Check<jmol>
   <jmolCheckbox>
-    <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/bg/2bge_consurf.spt"</scriptWhenChecked>
+    <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>
@@ Line 36: / Line 37: @@
 __TOC__
 </StructureSection>
+[[Category: Human]]
 [[Category: Protein-tyrosine-phosphatase]]
 [[Category: Black, E]]

2bge

From Proteopedia

Revision as of 06:42, 16 May 2018

Structure-based design of Protein Tyrosine Phosphatase-1B Inhibitors

Structural highlights

Function

Evolutionary Conservation

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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