1qxk: Difference between revisions
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New page: left|200px<br /> <applet load="1qxk" size="450" color="white" frame="true" align="right" spinBox="true" caption="1qxk, resolution 2.30Å" /> '''Monoacid-Based, Cel... |
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[[Image:1qxk.gif|left|200px]]<br /> | [[Image:1qxk.gif|left|200px]]<br /><applet load="1qxk" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="1qxk" size=" | |||
caption="1qxk, resolution 2.30Å" /> | caption="1qxk, resolution 2.30Å" /> | ||
'''Monoacid-Based, Cell Permeable, Selective Inhibitors of Protein Tyrosine Phosphatase 1B'''<br /> | '''Monoacid-Based, Cell Permeable, Selective Inhibitors of Protein Tyrosine Phosphatase 1B'''<br /> | ||
==Overview== | ==Overview== | ||
Monoacid-based PTP1B inhibitors with improved physiochemical properties | Monoacid-based PTP1B inhibitors with improved physiochemical properties have been investigated. A (2-hydroxy-phenoxy) acetic acid-based phosphotyrosyl mimetic has been linked with an optimized second arylphosphate binding site ligand to produce compound 20 with low micromolar potency against PTP1B, good selectivity over TCPTP (20-fold) and high cell permeability in the Caco-2 system. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
1QXK 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 429 as [http://en.wikipedia.org/wiki/ligand ligand]. 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:// | 1QXK 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=429:'>429</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=1QXK OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Abad-Zapatero, C.]] | [[Category: Abad-Zapatero, C.]] | ||
[[Category: Ballaron, S | [[Category: Ballaron, S J.]] | ||
[[Category: Hajduk, P | [[Category: Hajduk, P J.]] | ||
[[Category: Hutchins, C | [[Category: Hutchins, C W.]] | ||
[[Category: Jirousek, M | [[Category: Jirousek, M R.]] | ||
[[Category: Li, X.]] | [[Category: Li, X.]] | ||
[[Category: Liu, G.]] | [[Category: Liu, G.]] | ||
[[Category: Lubben, T | [[Category: Lubben, T H.]] | ||
[[Category: Pei, Z.]] | [[Category: Pei, Z.]] | ||
[[Category: Stashko, M | [[Category: Stashko, M A.]] | ||
[[Category: Szczepankiewick, B | [[Category: Szczepankiewick, B G.]] | ||
[[Category: Trevillyan, J | [[Category: Trevillyan, J M.]] | ||
[[Category: Xin, Z.]] | [[Category: Xin, Z.]] | ||
[[Category: Zhang, T.]] | [[Category: Zhang, T.]] | ||
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[[Category: ptp1b monoacid-based and cell permeable]] | [[Category: ptp1b monoacid-based and cell permeable]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:44:50 2008'' | ||
