2vex: Difference between revisions
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==Overview== | ==Overview== | ||
The structure-based design and synthesis of isothiazolidinone (IZD) | The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are interacting extensively with the B site of the enzyme. | ||
==Disease== | ==Disease== | ||
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[[Category: Protein-tyrosine-phosphatase]] | [[Category: Protein-tyrosine-phosphatase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Ala, P | [[Category: Ala, P J.]] | ||
[[Category: Bostrom, L.]] | [[Category: Bostrom, L.]] | ||
[[Category: Bower, M | [[Category: Bower, M J.]] | ||
[[Category: Burn, T | [[Category: Burn, T C.]] | ||
[[Category: Combs, A | [[Category: Combs, A P.]] | ||
[[Category: Douty, B.]] | [[Category: Douty, B.]] | ||
[[Category: Gonneville, L.]] | [[Category: Gonneville, L.]] | ||
[[Category: Klabe, R.]] | [[Category: Klabe, R.]] | ||
[[Category: Liu, P | [[Category: Liu, P C.C.]] | ||
[[Category: Pruitt, J.]] | [[Category: Pruitt, J.]] | ||
[[Category: Wayland, B.]] | [[Category: Wayland, B.]] | ||
[[Category: Wei, M.]] | [[Category: Wei, M.]] | ||
[[Category: Wynn, R.]] | [[Category: Wynn, R.]] | ||
[[Category: Yue, E | [[Category: Yue, E W.]] | ||
[[Category: IZ4]] | [[Category: IZ4]] | ||
[[Category: MG]] | [[Category: MG]] | ||
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[[Category: protein phosphatase]] | [[Category: protein phosphatase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:55:25 2008'' | ||
Revision as of 19:55, 21 February 2008
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CRYSTAL STRUCUTRE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR
OverviewOverview
The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are interacting extensively with the B site of the enzyme.
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
2VEX 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 Known structural/functional Sites: and . Full crystallographic information is available from OCA.
ReferenceReference
Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines., Douty B, Wayland B, Ala PJ, Bower MJ, Pruitt J, Bostrom L, Wei M, Klabe R, Gonneville L, Wynn R, Burn TC, Liu PC, Combs AP, Yue EW, Bioorg Med Chem Lett. 2008 Jan 1;18(1):66-71. Epub 2007 Nov 9. PMID:18037290
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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
- Ala, P J.
- Bostrom, L.
- Bower, M J.
- Burn, T C.
- Combs, A P.
- Douty, B.
- Gonneville, L.
- Klabe, R.
- Liu, P C.C.
- Pruitt, J.
- Wayland, B.
- Wei, M.
- Wynn, R.
- Yue, E W.
- IZ4
- MG
- Acetylation
- Endoplasmic reticulum
- Hydrolase
- Membrane
- Oxidation
- Phosphatase
- Phosphorylation
- Polymorphism
- Protein phosphatase