title: Design and synthesis of class-selective activity probes for protein tyrosine phosphatases.
abstract: Two mechanism-based activity probes, adopting a cassette-like design, for protein tyrosine phosphatases (PTPs) were synthesized. Both probes carry a phosphate group that serves as the recognition head for the target PTPs but differ in their reporter groups; probe LCL-1 uses a dansyl fluorophore, while LCL-2 has a biotin reporter group. LCL-1 and LCL-2 are specifically activated by phosphatase, leading to its covalent labeling, as exemplified with PTP-1B. However, they show no activation with other classes of hydrolases, including trypsin and beta-galactosidase. LCL-1 and LCL-2 thus represent the first example of class-selective probes for phosphatases.
authors.affiliation: Department of Chemistry, National Taiwan University, Taipei 106, Taiwan. lclo@ccms.ntu.edu.tw
authors.forename: Lee-Chiang
authors.initials: LC
authors.lastname: Lo
authors.forename: Te-Ling
authors.initials: TL
authors.lastname: Pang
authors.forename: Chi-Hsien
authors.initials: CH
authors.lastname: Kuo
authors.forename: Ying-Ling
authors.initials: YL
authors.lastname: Chiang
authors.forename: Hsin-Yi
authors.initials: HY
authors.lastname: Wang
authors.forename: Jing-Jer
authors.initials: JJ
authors.lastname: Lin
mesh_terms: D004789:Enzyme Activation; D015335:Molecular Probes / Q000138:chemical synthesis* / Q000737:chemistry*; D015394:Molecular Structure; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases / Q000737:chemistry / Q000378:metabolism*; D012680:Sensitivity and Specificity; D013379:Substrate Specificity
chemical_list: D015335:Molecular Probes; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases