2f6w

From Proteopedia

Protein tyrosine phosphatase 1B with sulfamic acid inhibitors

Structural highlights

2f6w is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 2.2Å
Ligands:	CL, MG, UN3
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

Checkto colour the structure by Evolutionary Conservation, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

Publication Abstract from PubMed

High-throughput screening of the P&GP corporate repository against several protein tyrosine phosphatases identified the sulfamic acid moiety as potential phosphotyrosine mimetic. Incorporation of the sulfamic acid onto a 1,2,3,4-tetrahydroisoquinoline scaffold provided a promising starting point for PTP1B inhibitor design.

1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors.,Klopfenstein SR, Evdokimov AG, Colson AO, Fairweather NT, Neuman JJ, Maier MB, Gray JL, Gerwe GS, Stake GE, Howard BW, Farmer JA, Pokross ME, Downs TR, Kasibhatla B, Peters KG Bioorg Med Chem Lett. 2006 Mar 15;16(6):1574-8. Epub 2006 Jan 4. PMID:16386905^[3]

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

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Citations

10 reviews cite this structure

Microfluidics: reframing biological enquiry.

Duncombe et al. (2015)

9 more

30 other articles

No citations found

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
↑ Klopfenstein SR, Evdokimov AG, Colson AO, Fairweather NT, Neuman JJ, Maier MB, Gray JL, Gerwe GS, Stake GE, Howard BW, Farmer JA, Pokross ME, Downs TR, Kasibhatla B, Peters KG. 1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1574-8. Epub 2006 Jan 4. PMID:16386905 doi:http://dx.doi.org/10.1016/j.bmcl.2005.12.051

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

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PDB ID 2f6w

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Categories: Homo sapiens | Large Structures | Evdokimov AG | Klopfenstein SR | Pokross ME

2f6w

From Proteopedia

Protein tyrosine phosphatase 1B with sulfamic acid inhibitors

Structural highlights

Function

Evolutionary Conservation

Publication Abstract from PubMed

See Also

References

Contents

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