title: Design and synthesis of paracaseolide A analogues as selective protein tyrosine phosphatase 1B inhibitors.
abstract: A series of structurally related analogues of the natural product paracaseolide A were synthesized and identified as potent PTP1B inhibitors. Among these analogues, compound 10 in particular showed improved PTP1B enzyme inhibitory activity, high selectivity for PTP1B over TC-PTP, and improved cellular effects.
authors.affiliation: State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, P.R. China. liying@lzu.edu.cn.
authors.forename: Jian-Peng
authors.initials: JP
authors.lastname: Yin
authors.forename: Chun-Lan
authors.initials: CL
authors.lastname: Tang
authors.forename: Li-Xin
authors.initials: LX
authors.lastname: Gao
authors.forename: Wei-Ping
authors.initials: WP
authors.lastname: Ma
authors.forename: Jing-Ya
authors.initials: JY
authors.lastname: Li
authors.forename: Ying
authors.initials: Y
authors.lastname: Li
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.forename: Fa-Jun
authors.initials: FJ
authors.lastname: Nan
mesh_terms: D015107:4-Butyrolactone / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007202:Indicators and Reagents; D007328:Insulin / Q000378:metabolism; D062105:Molecular Docking Simulation; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011972:Receptor, Insulin / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D007328:Insulin; C569208:paracaseolide A; D011972:Receptor, Insulin; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D015107:4-Butyrolactone