By imitating the scaffold of lithocholic acid (LCA), a natural steroidal compound displaying Protein Tyrosine Phosphatase 1B (PTP1B) inhibitory activity, a series of stilbene derivatives containing phenyl-substituted isoxazoles were designed and synthesized. The structures of the title compounds were confirmed by ¹H-NMR, 13C-NMR and HRMS. Activities of the title compounds were evaluated on PTP1...

Protein tyrosine phosphatase 1B (PTP1B) plays important role in diabetes, obesity and cancer. The methanol extract of the gum resin of Garcinia hanburyi (G. hanburyi) showed potent PTP1B inhibition at 10µg/ml. The active compounds were identified as prenylated caged xanthones (1-9) which inhibited PTP1B in dose-dependent manner. Carboxybutenyl group within caged motif (A ring) was found to play...

Interleukin-5 (IL-5) regulates the growth and function of eosinophils. It induces rapid tyrosine phosphorylation of Lyn and Jak2 tyrosine kinases. The role of tyrosine phosphatases in IL-5 signal transduction has not been investigated. In this study, we provide first evidence that SH2 protein tyrosine phosphatase 2 (SHPTP2) phosphotyrosine phosphatase plays a key role in prevention of eosinophi...

Serum albumin secretion from rat hepatocytes proceeds via the constitutive pathway. Although much is known about the role of protein tyrosine phosphorylation in regulated secretion, nothing is known about its function in the constitutive process. Here we show that albumin secretion is inhibited by the tyrosine kinase inhibitor genistein but relatively insensitive to subtype-selective inhibitors...

We report that the activity of a rationally engineered protein tyrosine phosphatase (PTP) mutant can be fully rescued by the addition of the biarsenical fluorescein derivative FlAsH, a compound that does not affect the activity of wild-type PTPs.

Purification and characterization of ZmRIP1, a novel 1 reductant-inhibited protein tyrosine phosphatase from maize 2 Bingbing Li, Yanxia Zhao ,Liyan Liang, Huibo Ren, Yu Xing, Lin 3 Chen, Mingzhu Sun , Yuanhua Wang , Yu Han , Haifeng Jia , Conglin 4 Huang, Zhongyi Wu and Wensuo Jia 5 College of Agronomy and Biotechnology, China Agricultural University, Beijing, China 6 Beijing Agro-Biotechnolog...

Review on PTPRA, with data on DNA/RNA expression, on the protein encoded, and the functional importance of the gene.

The protein-tyrosine phosphatase (PTP) 'YopH' is a virulence factor of Yersinia pestis, the causative agent of plague. Potential use of Yersinia as a bioterrorism agent renders YopH inhibitors of therapeutic importance. Previously, we had examined the inhibitory potencies of a variety of phosphotyrosyl (pTyr) mimetics against the human PTP1B enzyme by displaying them in the EGFR-derived hexapep...

Protein tyrosine phosphatases act in conjunction with protein kinases to regulate the tyrosine phosphorylation events that control cell activation and differentiation. We have isolated a previously undescribed human phosphatase, Lyp, that encodes an intracellular 105-kD protein containing a single tyrosine phosphatase catalytic domain. The noncatalytic domain contains four proline-rich potentia...