2vev

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[[Image:2vev.jpg|left|200px]]<br /><applet load="2vev" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2vev.jpg|left|200px]]
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caption="2vev, resolution 1.8&Aring;" />
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'''CRYSTAL STRUCUTRE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR'''<br />
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{{Structure
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|PDB= 2vev |SIZE=350|CAPTION= <scene name='initialview01'>2vev</scene>, resolution 1.8&Aring;
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|SITE= <scene name='pdbsite=AC1:Iz2+Binding+Site+For+Chain+A'>AC1</scene> and <scene name='pdbsite=AC2:Mg+Binding+Site+For+Chain+A'>AC2</scene>
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|LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene> and <scene name='pdbligand=IZ2:N-[(1S)-1-(4-benzyl-1H-imidazol-2-yl)-2-{4-[(5S)-1,1-dioxido-3-oxoisothiazolidin-5-yl]phenyl}ethyl]-3-(trifluoromethyl)benzenesulfonamide'>IZ2</scene>
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|ACTIVITY= [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]
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|GENE=
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}}
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'''CRYSTAL STRUCUTRE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2VEV 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> and <scene name='pdbligand=IZ2:'>IZ2</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] Known structural/functional Sites: <scene name='pdbsite=AC1:Iz2+Binding+Site+For+Chain+A'>AC1</scene> and <scene name='pdbsite=AC2:Mg+Binding+Site+For+Chain+A'>AC2</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2VEV OCA].
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2VEV is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2VEV OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=18037290 18037290]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/18037290 18037290]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein-tyrosine-phosphatase]]
[[Category: Protein-tyrosine-phosphatase]]
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[[Category: protein phosphatase]]
[[Category: protein phosphatase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:55:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:45:55 2008''

Revision as of 16:45, 20 March 2008

Image:2vev.jpg


PDB ID 2vev

Drag the structure with the mouse to rotate
, resolution 1.8Å
Sites: and
Ligands: and
Activity: Protein-tyrosine-phosphatase, with EC number 3.1.3.48
Coordinates: save as pdb, mmCIF, xml



CRYSTAL STRUCUTRE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR


Contents

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.

Disease

Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]

About this Structure

2VEV is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

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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