2azr: Difference between revisions
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New page: left|200px<br /> <applet load="2azr" size="450" color="white" frame="true" align="right" spinBox="true" caption="2azr, resolution 2.0Å" /> '''Crystal structure of... |
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[[Image:2azr.gif|left|200px]]<br /> | [[Image:2azr.gif|left|200px]]<br /><applet load="2azr" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2azr" size=" | |||
caption="2azr, resolution 2.0Å" /> | caption="2azr, resolution 2.0Å" /> | ||
'''Crystal structure of PTP1B with Bicyclic Thiophene inhibitor'''<br /> | '''Crystal structure of PTP1B with Bicyclic Thiophene inhibitor'''<br /> | ||
==Overview== | ==Overview== | ||
A novel pyridothiophene inhibitor of PTP1B was discovered by rational | A novel pyridothiophene inhibitor of PTP1B was discovered by rational screening of phosphotyrosine mimics at high micromolar concentrations. The potency of this lead compound has been improved significantly by medicinal chemistry guided by X-ray crystallography and molecular modeling. Excellent consistency has been observed between structure-activity relationships and structural information from PTP1B-inhibitor complexes. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
2AZR 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 982 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:// | 2AZR 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=982:'>982</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=2AZR OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Binnun, E.]] | [[Category: Binnun, E.]] | ||
[[Category: Erbe, D | [[Category: Erbe, D V.]] | ||
[[Category: Follows, B | [[Category: Follows, B C.]] | ||
[[Category: Foreman, K.]] | [[Category: Foreman, K.]] | ||
[[Category: Joseph-McCarthy, D.]] | [[Category: Joseph-McCarthy, D.]] | ||
[[Category: Kirincich, S | [[Category: Kirincich, S J.]] | ||
[[Category: Lee, J.]] | [[Category: Lee, J.]] | ||
[[Category: Moretto, A | [[Category: Moretto, A F.]] | ||
[[Category: Smith, M | [[Category: Smith, M J.]] | ||
[[Category: Tam, S | [[Category: Tam, S K.]] | ||
[[Category: Tam, S | [[Category: Tam, S Y.]] | ||
[[Category: Wan, Z | [[Category: Wan, Z K.]] | ||
[[Category: Wilson, D | [[Category: Wilson, D P.]] | ||
[[Category: Xu, W | [[Category: Xu, W X.]] | ||
[[Category: Zhang, Y | [[Category: Zhang, Y L.]] | ||
[[Category: 982]] | [[Category: 982]] | ||
[[Category: bicyclic thiophenes]] | [[Category: bicyclic thiophenes]] | ||
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[[Category: protein tyrosine phosphatase]] | [[Category: protein tyrosine phosphatase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:32:42 2008'' | ||
