2vey: Difference between revisions
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==Overview== | ==Overview== | ||
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. | 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== | |||
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=176885 176885]], Insulin resistance, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=176885 176885]] | |||
==About this Structure== | ==About this Structure== | ||
2VEY 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=IZ5:'>IZ5</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] Known structural/functional Site: <scene name='pdbsite=AC1:Iz5 Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2VEY OCA]. | 2VEY 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=IZ5:'>IZ5</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] Known structural/functional Site: <scene name='pdbsite=AC1:Iz5+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2VEY OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: protein phosphatase]] | [[Category: protein phosphatase]] | ||
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Revision as of 11:51, 3 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
2VEY 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 Known structural/functional Site: . 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.
- IZ5
- Acetylation
- Endoplasmic reticulum
- Hydrolase
- Membrane
- Oxidation
- Phosphatase
- Phosphorylation
- Polymorphism
- Protein phosphatase