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1q1m
From Proteopedia
(New page: 200px<br /> <applet load="1q1m" size="450" color="white" frame="true" align="right" spinBox="true" caption="1q1m, resolution 2.60Å" /> '''A Highly Efficient ...) |
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| - | [[Image:1q1m. | + | [[Image:1q1m.jpg|left|200px]]<br /><applet load="1q1m" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1q1m, resolution 2.60Å" /> | caption="1q1m, resolution 2.60Å" /> | ||
'''A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors'''<br /> | '''A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1Q1M 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 234 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:// | + | 1Q1M 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=234:'>234</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=1Q1M OCA]. |
==Reference== | ==Reference== | ||
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[[Category: ptp1b]] | [[Category: ptp1b]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:42:18 2008'' |
Revision as of 14:42, 15 February 2008
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A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors
Contents |
Overview
Using an NMR-based fragment screening and X-ray crystal structure-based, assembly, starting with millimolar ligands for both the catalytic site and, the second phosphotyrosine binding site, we have identified a, small-molecule inhibitor of protein tyrosine phosphatase 1B with low, micromolar inhibition constant, high selectivity (30-fold) over the highly, homologous T-cell protein tyrosine phosphatase, and good cellular activity, in COS-7 cells.
Disease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this Structure
1Q1M 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 Full crystallographic information is available from OCA.
Reference
Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor., Liu G, Xin Z, Pei Z, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Zhao H, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR, J Med Chem. 2003 Sep 25;46(20):4232-5. PMID:13678400
Page seeded by OCA on Fri Feb 15 16:42:18 2008
Categories: Homo sapiens | Protein-tyrosine-phosphatase | Single protein | Abad-Zapatero, C. | Ballaron, S.J. | Haasch, D.L. | Hajduk, P.J. | Hutchins, C.W. | Jirousek, M.R. | Kaszubska, W. | Liu, G. | Lubben, T.H. | Pei, Z. | Rondinone, C.M. | Trevillyan, J.M. | Xin, Z. | Zhao, H. | 234 | Inhibitors with isoxazole-salicylate pharmacophores | Protein tyrosine phosphatase 1b | Ptp1b
