title: Discovery of a novel submicromolar inhibitor of the lymphoid specific tyrosine phosphatase.
abstract: We report here a class of thiazolidine-2,4-diones and 2-thioxothiazolidin-4-ones as potent inhibitors of the lymphoid specific tyrosine phosphatase (Lyp) identified from high throughput screens. Chemical modification by incorporating the known phosphotyrosine (pTyr) mimics led to the discovery of a salicylate-based inhibitor with submicromolar potency.
authors.affiliation: Department of Medicine, Columbia University, 650 W 168th Street, BB 1029, New York, NY 10032, USA.
authors.forename: Yuli
authors.initials: Y
authors.lastname: Xie
authors.forename: Yidong
authors.initials: Y
authors.lastname: Liu
authors.forename: Gangli
authors.initials: G
authors.lastname: Gong
authors.forename: Alison
authors.initials: A
authors.lastname: Rinderspacher
authors.forename: Shi-Xian
authors.initials: SX
authors.lastname: Deng
authors.forename: Deborah H
authors.initials: DH
authors.lastname: Smith
authors.forename: Udo
authors.initials: U
authors.lastname: Toebben
authors.forename: Effie
authors.initials: E
authors.lastname: Tzilianos
authors.forename: Lars
authors.initials: L
authors.lastname: Branden
authors.forename: Dusica
authors.initials: D
authors.lastname: Vidović
authors.forename: Caty
authors.initials: C
authors.lastname: Chung
authors.forename: Stephan
authors.initials: S
authors.lastname: Schürer
authors.forename: Lutz
authors.initials: L
authors.lastname: Tautz
authors.forename: Donald W
authors.initials: DW
authors.lastname: Landry
mesh_terms: D001665:Binding Sites; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D008956:Models, Chemical; D018716:Molecular Mimicry; D019000:Phosphotyrosine / Q000737:chemistry; D054596:Protein Tyrosine Phosphatase, Non-Receptor Type 22 / Q000037:antagonists & inhibitors*; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000494:pharmacology*; D053778:Thiazolidines / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D045162:Thiazolidinediones; D053778:Thiazolidines; D019000:Phosphotyrosine; D054596:Protein Tyrosine Phosphatase, Non-Receptor Type 22; D017027:Protein Tyrosine Phosphatases