2vew: Difference between revisions

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|PDB= 2vew |SIZE=350|CAPTION= <scene name='initialview01'>2vew</scene>, resolution 2.0&Aring;
|PDB= 2vew |SIZE=350|CAPTION= <scene name='initialview01'>2vew</scene>, resolution 2.0&Aring;
|SITE= <scene name='pdbsite=AC1:Iz3+Binding+Site+For+Chain+A'>AC1</scene> and <scene name='pdbsite=AC2:Mg+Binding+Site+For+Chain+A'>AC2</scene>
|SITE= <scene name='pdbsite=AC1:Iz3+Binding+Site+For+Chain+A'>AC1</scene> and <scene name='pdbsite=AC2:Mg+Binding+Site+For+Chain+A'>AC2</scene>
|LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene> and <scene name='pdbligand=IZ3:3-fluoro-N-[(1S)-1-[4-[(2-fluorophenyl)methyl]imidazol-2-yl]-2-[4-[(5S)-1,1,3-trioxo-1,2-thiazolidin-5-yl]phenyl]ethyl]benzenesulfonamide'>IZ3</scene>
|LIGAND= <scene name='pdbligand=IZ3:3-FLUORO-N-[(1S)-1-[4-[(2-FLUOROPHENYL)METHYL]IMIDAZOL-2-YL]-2-[4-[(5S)-1,1,3-TRIOXO-1,2-THIAZOLIDIN-5-YL]PHENYL]ETHYL]BENZENESULFONAMIDE'>IZ3</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>
|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]  
|ACTIVITY= <span class='plainlinks'>[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] </span>
|GENE=  
|GENE=  
|DOMAIN=
|RELATEDENTRY=[[2f6t|2F6T]], [[2f6f|2F6F]], [[2cnf|2CNF]], [[2cm3|2CM3]], [[2cm2|2CM2]], [[1g1f|1G1F]], [[1q6n|1Q6N]], [[1ptu|1PTU]], [[1c84|1C84]], [[2veu|2VEU]], [[1q1m|1Q1M]], [[1nz7|1NZ7]], [[2azr|2AZR]], [[1c88|1C88]], [[1oet|1OET]], [[1c83|1C83]], [[1sug|1SUG]], [[1onz|1ONZ]], [[2cnh|2CNH]], [[1xbo|1XBO]], [[1ptv|1PTV]], [[1g1g|1G1G]], [[2hnp|2HNP]], [[1t49|1T49]], [[1nwl|1NWL]], [[2f6y|2F6Y]], [[2cne|2CNE]], [[1nl9|1NL9]], [[1c86|1C86]], [[1kav|1KAV]], [[2hnq|2HNQ]], [[1jf7|1JF7]], [[1pxh|1PXH]], [[1q6s|1Q6S]], [[1l8g|1L8G]], [[2cma|2CMA]], [[1q6m|1Q6M]], [[1bzj|1BZJ]], [[1i57|1I57]], [[1wax|1WAX]], [[1ony|1ONY]], [[1g1h|1G1H]], [[2cng|2CNG]], [[1t4j|1T4J]], [[1kak|1KAK]], [[2cni|2CNI]], [[2b07|2B07]], [[2cm8|2CM8]], [[1eeo|1EEO]], [[1g7g|1G7G]], [[1ptt|1PTT]], [[1qxk|1QXK]], [[1ecv|1ECV]], [[1oem|1OEM]], [[2cmb|2CMB]], [[1nwe|1NWE]], [[2fjn|2FJN]], [[1aax|1AAX]], [[2vev|2VEV]], [[2vey|2VEY]], [[2b4s|2B4S]], [[2cm7|2CM7]], [[2bgd|2BGD]], [[2vex|2VEX]], [[1a5y|1A5Y]], [[2cmc|2CMC]], [[1c85|1C85]], [[1lqf|1LQF]], [[2f6w|2F6W]], [[1c87|1C87]], [[1no6|1NO6]], [[1pyn|1PYN]], [[2bge|2BGE]], [[1oes|1OES]], [[1bzc|1BZC]], [[2f6z|2F6Z]], [[2f71|2F71]], [[1oeu|1OEU]], [[1q6t|1Q6T]], [[1g7f|1G7F]], [[1nny|1NNY]], [[2f70|2F70]], [[1q6j|1Q6J]], [[1q6p|1Q6P]], [[2f6v|2F6V]], [[1t48|1T48]], [[2fjm|2FJM]], [[1oeo|1OEO]], [[1pa1|1PA1]], [[1ph0|1PH0]], [[1bzh|1BZH]], [[1gfy|1GFY]], [[1een|1EEN]], [[1oev|1OEV]], [[1pty|1PTY]]
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2vew FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vew OCA], [http://www.ebi.ac.uk/pdbsum/2vew PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2vew RCSB]</span>
}}
}}


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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==
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[[Category: Wynn, R.]]
[[Category: Wynn, R.]]
[[Category: Yue, E W.]]
[[Category: Yue, E W.]]
[[Category: IZ3]]
[[Category: MG]]
[[Category: acetylation]]
[[Category: acetylation]]
[[Category: endoplasmic reticulum]]
[[Category: endoplasmic reticulum]]
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[[Category: protein phosphatase]]
[[Category: protein phosphatase]]


''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:45:51 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:11:29 2008''