1ph0
From Proteopedia
(New page: 200px<br /> <applet load="1ph0" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ph0, resolution 2.20Å" /> '''Non-carboxylic Acid...) |
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caption="1ph0, resolution 2.20Å" /> | caption="1ph0, resolution 2.20Å" /> | ||
'''Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site'''<br /> | '''Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1PH0 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 418 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:// | + | 1PH0 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=418:'>418</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=1PH0 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: salicylic acid moiety at the second site]] | [[Category: salicylic acid moiety at the second site]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:40:03 2008'' |
Revision as of 14:40, 15 February 2008
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Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site
Contents |
Overview
Protein tyrosine phosphatase (PTPase) 1B (PTP1B) has been implicated as a, key negative regulator of both insulin and leptin signaling cascades. We, identified several salicylic acid-based ligands for the second, phosphotyrosine binding site of PTP1B using a NMR-based screening., Structure-based linking with a catalytic site-directed, oxalylarylaminobenzoic acid-based pharmacophore led to the identification, of a novel series of potent PTP1B inhibitors exhibiting 6-fold selectivity, over the highly homologous T-cell PTPase (TCPTP) and high selectivity over, other phosphatases.
Disease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this Structure
1PH0 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
Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands., Liu G, Xin Z, Liang H, Abad-Zapatero C, Hajduk PJ, Janowick DA, Szczepankiewicz BG, Pei Z, Hutchins CW, Ballaron SJ, Stashko MA, Lubben TH, Berg CE, Rondinone CM, Trevillyan JM, Jirousek MR, J Med Chem. 2003 Jul 31;46(16):3437-40. PMID:12877578
Page seeded by OCA on Fri Feb 15 16:40:03 2008
Categories: Homo sapiens | Protein-tyrosine-phosphatase | Single protein | Abad-Zapatero, C. | Ballaron, S.J. | Hajduk, P. | Hutchins, C.W. | Janowick, D. | Liang, H. | Liu, G. | Pei, Z. | Szczepankiewicz, B. | Xin, Z. | 418 | Oxalyl-aryl-benzoic acid compound inhibitor | Protein tyrosine phosphatase 1b | Salicylic acid moiety at the second site
