2f70: Difference between revisions
New page: left|200px<br /> <applet load="2f70" size="450" color="white" frame="true" align="right" spinBox="true" caption="2f70, resolution 2.120Å" /> '''Protein tyrosine p... |
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[[Image:2f70.gif|left|200px]]<br /> | [[Image:2f70.gif|left|200px]]<br /><applet load="2f70" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="2f70, resolution 2.120Å" /> | caption="2f70, resolution 2.120Å" /> | ||
'''Protein tyrosine phosphatase 1B with sulfamic acid inhibitors'''<br /> | '''Protein tyrosine phosphatase 1B with sulfamic acid inhibitors'''<br /> | ||
==Overview== | ==Overview== | ||
High-throughput screening of the P&GP corporate repository against several | 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. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
2F70 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with MG, CL and UN6 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http:// | 2F70 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=CL:'>CL</scene> and <scene name='pdbligand=UN6:'>UN6</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2F70 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Protein-tyrosine-phosphatase]] | [[Category: Protein-tyrosine-phosphatase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Evdokimov, A | [[Category: Evdokimov, A G.]] | ||
[[Category: Klopfenstein, S | [[Category: Klopfenstein, S R.]] | ||
[[Category: Pokross, M | [[Category: Pokross, M E.]] | ||
[[Category: CL]] | [[Category: CL]] | ||
[[Category: MG]] | [[Category: MG]] | ||
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[[Category: tyrosine]] | [[Category: tyrosine]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:18:21 2008'' | ||
Revision as of 18:18, 21 February 2008
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Protein tyrosine phosphatase 1B with sulfamic acid inhibitors
OverviewOverview
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.
DiseaseDisease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this StructureAbout this Structure
2F70 is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Protein-tyrosine-phosphatase, with EC number 3.1.3.48 Full crystallographic information is available from OCA.
ReferenceReference
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
Page seeded by OCA on Thu Feb 21 17:18:21 2008