1qxk: Difference between revisions
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'' | ||
Revision as of 15:44, 21 February 2008
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Monoacid-Based, Cell Permeable, Selective Inhibitors of Protein Tyrosine Phosphatase 1B
OverviewOverview
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.
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
1QXK is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Protein-tyrosine-phosphatase, with EC number 3.1.3.48 Full crystallographic information is available from OCA.
ReferenceReference
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B., Xin Z, Liu G, Abad-Zapatero C, Pei Z, Szczepankiewicz BG, Li X, Zhang T, Hutchins CW, Hajduk PJ, Ballaron SJ, Stashko MA, Lubben TH, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2003 Nov 17;13(22):3947-50. PMID:14592481
Page seeded by OCA on Thu Feb 21 14:44:50 2008
Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- Homo sapiens
- Protein-tyrosine-phosphatase
- Single protein
- Abad-Zapatero, C.
- Ballaron, S J.
- Hajduk, P J.
- Hutchins, C W.
- Jirousek, M R.
- Li, X.
- Liu, G.
- Lubben, T H.
- Pei, Z.
- Stashko, M A.
- Szczepankiewick, B G.
- Trevillyan, J M.
- Xin, Z.
- Zhang, T.
- 429
- Protein tyrosine phosphatase 1b
- Ptp1b monoacid-based and cell permeable