3d9c

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Crystal Structure PTP1B complex with aryl Seleninic acidCrystal Structure PTP1B complex with aryl Seleninic acid

Structural highlights

3d9c 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:
Gene:PTPN1, PTP1B (HUMAN)
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

A homotyrosine based seleninic acid irreversibly inhibits protein tyrosine phosphatases by forming a covalent selenosulfide linkage with the active site cysteine sulfhydryl specifically. The details of the event are revealed by model synthetic studies and by kinetic, mass spectrometric, and crystallographic characterization.

Seleninate in place of phosphate: irreversible inhibition of protein tyrosine phosphatases.,Abdo M, Liu S, Zhou B, Walls CD, Wu L, Knapp S, Zhang ZY J Am Chem Soc. 2008 Oct 8;130(40):13196-7. Epub 2008 Sep 10. PMID:18781746[3]

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

See Also

References

  1. ↑ 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
  2. ↑ 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
  3. ↑ Abdo M, Liu S, Zhou B, Walls CD, Wu L, Knapp S, Zhang ZY. Seleninate in place of phosphate: irreversible inhibition of protein tyrosine phosphatases. J Am Chem Soc. 2008 Oct 8;130(40):13196-7. Epub 2008 Sep 10. PMID:18781746 doi:10.1021/ja804489m

3d9c, resolution 2.30Å

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