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2vex

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Revision as of 09:42, 18 November 2020

CRYSTAL STRUCTURE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR

Structural highlights

2vex 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:	2f6t, 2f6f, 2cnf, 2cm3, 2cm2, 1g1f, 1q6n, 1ptu, 1c84, 2veu, 1q1m, 1nz7, 2azr, 1c88, 1oet, 1c83, 1sug, 1onz, 1ptv, 2cnh, 1xbo, 1g1g, 2hnp, 1t49, 1nwl, 2f6y, 2cne, 1nl9, 1c86, 1kav, 2hnq, 1jf7, 1pxh, 1q6s, 1l8g, 2cma, 1q6m, 1i57, 1bzj, 1wax, 1ony, 1g1h, 2cng, 1t4j, 1kak, 2cni, 2b07, 2cm8, 1eeo, 1ptt, 1g7g, 1qxk, 1ecv, 1oem, 2cmb, 1nwe, 2fjn, 1aax, 2vev, 2vey, 2b4s, 2bgd, 2cm7, 1a5y, 2cmc, 1c85, 1lqf, 1c87, 2f6w, 1no6, 1pyn, 2bge, 1oes, 1bzc, 2f6z, 2f71, 1q6t, 1oeu, 1g7f, 1nny, 1q6j, 2f70, 1q6p, 2f6v, 1t48, 2fjm, 1oeo, 1pa1, 1ph0, 1bzh, 1gfy, 1een, 1pty, 1oev
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

The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are interacting extensively with the B site of the enzyme.

Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.,Douty B, Wayland B, Ala PJ, Bower MJ, Pruitt J, Bostrom L, Wei M, Klabe R, Gonneville L, Wynn R, Burn TC, Liu PC, Combs AP, Yue EW Bioorg Med Chem Lett. 2008 Jan 1;18(1):66-71. Epub 2007 Nov 9. PMID:18037290^[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
↑ Douty B, Wayland B, Ala PJ, Bower MJ, Pruitt J, Bostrom L, Wei M, Klabe R, Gonneville L, Wynn R, Burn TC, Liu PC, Combs AP, Yue EW. Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines. Bioorg Med Chem Lett. 2008 Jan 1;18(1):66-71. Epub 2007 Nov 9. PMID:18037290 doi:10.1016/j.bmcl.2007.11.012

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/2vex"

@@ Line 1: / Line 1: @@
-==CRYSTAL STRUCUTRE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR==
+==CRYSTAL STRUCTURE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR==
 <StructureSection load='2vex' size='340' side='right'caption='[[2vex]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[2vex]] 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=2VEX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2VEX FirstGlance]. <br>
+<table><tr><td colspan='2'>[[2vex]] 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=2VEX OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=2VEX FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=IZ4:N-{(1S)-2-{4-[(5S)-1,1-DIOXIDO-3-OXOISOTHIAZOLIDIN-5-YL]PHENYL}-1-[(4R)-4-(2-PHENYLETHYL)-4,5-DIHYDRO-1H-IMIDAZOL-2-YL]ETHYL}-3-FLUOROBENZENESULFONAMIDE'>IZ4</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
+</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=IZ4:N-{(1S)-2-{4-[(5S)-1,1-DIOXIDO-3-OXOISOTHIAZOLIDIN-5-YL]PHENYL}-1-[(4R)-4-(2-PHENYLETHYL)-4,5-DIHYDRO-1H-IMIDAZOL-2-YL]ETHYL}-3-FLUOROBENZENESULFONAMIDE'>IZ4</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
 <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2f6t|2f6t]], [[2f6f|2f6f]], [[2cnf|2cnf]], [[2cm3|2cm3]], [[2cm2|2cm2]], [[1g1f|1g1f]], [[1q6n|1q6n]], [[1ptu|1ptu]], [[1c84|1c84]], [[2veu|2veu]], [[1q1m|1q1m]], [[1nz7|1nz7]], [[2azr|2azr]], [[1c88|1c88]], [[1oet|1oet]], [[1c83|1c83]], [[1sug|1sug]], [[1onz|1onz]], [[1ptv|1ptv]], [[2cnh|2cnh]], [[1xbo|1xbo]], [[1g1g|1g1g]], [[2hnp|2hnp]], [[1t49|1t49]], [[1nwl|1nwl]], [[2f6y|2f6y]], [[2cne|2cne]], [[1nl9|1nl9]], [[1c86|1c86]], [[1kav|1kav]], [[2hnq|2hnq]], [[1jf7|1jf7]], [[1pxh|1pxh]], [[1q6s|1q6s]], [[1l8g|1l8g]], [[2cma|2cma]], [[1q6m|1q6m]], [[1i57|1i57]], [[1bzj|1bzj]], [[1wax|1wax]], [[1ony|1ony]], [[1g1h|1g1h]], [[2cng|2cng]], [[1t4j|1t4j]], [[1kak|1kak]], [[2cni|2cni]], [[2b07|2b07]], [[2cm8|2cm8]], [[1eeo|1eeo]], [[1ptt|1ptt]], [[1g7g|1g7g]], [[1qxk|1qxk]], [[1ecv|1ecv]], [[1oem|1oem]], [[2cmb|2cmb]], [[1nwe|1nwe]], [[2fjn|2fjn]], [[1aax|1aax]], [[2vev|2vev]], [[2vey|2vey]], [[2b4s|2b4s]], [[2bgd|2bgd]], [[2cm7|2cm7]], [[1a5y|1a5y]], [[2cmc|2cmc]], [[1c85|1c85]], [[1lqf|1lqf]], [[1c87|1c87]], [[2f6w|2f6w]], [[1no6|1no6]], [[1pyn|1pyn]], [[2bge|2bge]], [[1oes|1oes]], [[1bzc|1bzc]], [[2f6z|2f6z]], [[2f71|2f71]], [[1q6t|1q6t]], [[1oeu|1oeu]], [[1g7f|1g7f]], [[1nny|1nny]], [[1q6j|1q6j]], [[2f70|2f70]], [[1q6p|1q6p]], [[2f6v|2f6v]], [[1t48|1t48]], [[2fjm|2fjm]], [[1oeo|1oeo]], [[1pa1|1pa1]], [[1ph0|1ph0]], [[1bzh|1bzh]], [[1gfy|1gfy]], [[1een|1een]], [[1pty|1pty]], [[1oev|1oev]]</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=2vex FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vex OCA], [http://pdbe.org/2vex PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2vex RCSB], [http://www.ebi.ac.uk/pdbsum/2vex PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2vex ProSAT]</span></td></tr>
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=2vex FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vex OCA], [http://pdbe.org/2vex PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2vex RCSB], [http://www.ebi.ac.uk/pdbsum/2vex PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2vex ProSAT]</span></td></tr>
 </table>
 == Function ==
@@ Line 32: / Line 32: @@
 ==See Also==
-*[[Tyrosine phosphatase|Tyrosine phosphatase]]
+*[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]]
 == References ==
 <references/>

2vex

From Proteopedia

Revision as of 09:42, 18 November 2020

CRYSTAL STRUCTURE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR

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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