1ph0: Difference between revisions
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'''Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site''' | '''Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site''' | ||
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[[Category: Szczepankiewicz, B.]] | [[Category: Szczepankiewicz, B.]] | ||
[[Category: Xin, Z.]] | [[Category: Xin, Z.]] | ||
[[Category: | [[Category: Oxalyl-aryl-benzoic acid compound inhibitor]] | ||
[[Category: | [[Category: Protein tyrosine phosphatase 1b]] | ||
[[Category: | [[Category: Salicylic acid moiety at the second site]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:04:34 2008'' | |||
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Revision as of 02:04, 3 May 2008
Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site
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.
About this Structure
1PH0 is a Single protein structure of sequence from Homo sapiens. 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 Sat May 3 05:04:34 2008
Proteopedia Page Contributors and Editors (what is this?)
- 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.
- Oxalyl-aryl-benzoic acid compound inhibitor
- Protein tyrosine phosphatase 1b
- Salicylic acid moiety at the second site
