1ph0: Difference between revisions
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==Overview== | ==Overview== | ||
Protein tyrosine phosphatase (PTPase) 1B (PTP1B) has been implicated as a | 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== | ==Disease== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Abad-Zapatero, C.]] | [[Category: Abad-Zapatero, C.]] | ||
[[Category: Ballaron, S | [[Category: Ballaron, S J.]] | ||
[[Category: Hajduk, P.]] | [[Category: Hajduk, P.]] | ||
[[Category: Hutchins, C | [[Category: Hutchins, C W.]] | ||
[[Category: Janowick, D.]] | [[Category: Janowick, D.]] | ||
[[Category: Liang, H.]] | [[Category: Liang, H.]] | ||
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[[Category: salicylic acid moiety at the second site]] | [[Category: salicylic acid moiety at the second site]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:28:41 2008'' | ||