1ph0: Difference between revisions
New page: left|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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[[Image:1ph0. | [[Image:1ph0.jpg|left|200px]]<br /><applet load="1ph0" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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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 17:40, 15 February 2008
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Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site
OverviewOverview
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.
DiseaseDisease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this StructureAbout 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.
ReferenceReference
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
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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- 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