title: Quinoxalinylurea derivatives as a novel class of JSP-1 inhibitors.
abstract: A series of quinoxalinylurea-based inhibitors are synthesized and shown to be the novel and potent inhibitors against Jnk Stimulatory Phosphatase-1 (JSP-1), which is a special member of dual-specificity protein phosphatase (DSP) family. Biological assay and computational modeling studies showed the compounds were reversible and noncompetitive inhibitors of JSP-1. JSP-1 inhibitors may be useful for the treatment of inflammatory, vascular, neurodegenerative, metabolic, and oncological diseases in humans associated with dysfunctional Jnk signaling.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China.
authors.forename: Li
authors.initials: L
authors.lastname: Zhang
authors.forename: Beiying
authors.initials: B
authors.lastname: Qiu
authors.forename: Bing
authors.initials: B
authors.lastname: Xiong
authors.forename: Xin
authors.initials: X
authors.lastname: Li
authors.forename: Jingya
authors.initials: J
authors.lastname: Li
authors.forename: Xin
authors.initials: X
authors.lastname: Wang
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.forename: Jingkang
authors.initials: J
authors.lastname: Shen
mesh_terms: D000495:Allosteric Site; D054637:Dual-Specificity Phosphatases; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D054639:Mitogen-Activated Protein Kinase Phosphatases; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors*; D054645:Protein Phosphatase 1; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014508:Urea / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D011810:Quinoxalines; D014508:Urea; D054639:Mitogen-Activated Protein Kinase Phosphatases; D010749:Phosphoprotein Phosphatases; D054645:Protein Phosphatase 1; C442824:DUSP22 protein, human; D054637:Dual-Specificity Phosphatases; D017027:Protein Tyrosine Phosphatases