HA130 is a boronic acid based inhibitor of the lysoPLD activity of autotaxin (ATX). HA130 is a potent (IC₅₀ = 28 nM), reversible inhibitor which interacts with the oxygen in active site residue T210. HA130 is selective against ATX and does not show any activity against NPP1, alkaline phosphatase, phosphodiesterase, at concentrations up to 10 microM. In addition, proteosomal chymotryptic, caspase, and typtic activities were not affected. It also showed minimal toxicity against A2058, HEK293T, and HepG2 cell lines (TD₅₀ = 105, 83, & 2056 µM respectively). Plasma ATX activity was inhibited and circulating LPA levels decreased when administered to mice.

References

Powered by Bioz See more details on Bioz

1) H.M.H.G. Albers et al. “Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation” Proc. Natl. Acad. Sci. USA, 2010, 107, 7257-7262.2) H.M.H.G. Albers et al. “Discovery and Optimization of Boronic Acid Based Inhibitors of Autotaxin” J.Med. Chem., 2010, 53, 4958-4967.

Echelon-脂类研究的最佳拍档

Echelon是脂质研究和脂质与蛋白质相互作用研究领域的引导者。脂质蛋白相互作用是众多的细胞信号通路钟高级调控必不可少的。异常的细胞信号通路将会导致许多疾病，例如癌症、炎症、糖尿病和心血管疾病等。Echelon一直是脂质研究信息，脂质信号分析的顶级供应商。