Activity-based proteome profiling of potential cellular targets of orlistat− an FDA-approved drug with anti-tumor activities

…, MH Ngai, MJ Lear, MR Wenk, SQ Yao

Index: Yang, Peng-Yu; Liu, Kai; Ngai, Mun Hong; Lear, Martin J.; Wenk, Markus R.; Yao, Shao Q. Journal of the American Chemical Society, 2010 , vol. 132, # 2 p. 656 - 666

Full Text: HTML

Citation Number: 141

Abstract

Orlistat, or tetrahydrolipstatin (THL), is an FDA-approved antiobesity drug with potential antitumor activities. Cellular off-targets and potential side effects of Orlistat in cancer therapies, however, have not been extensively explored thus far. In this study, we report the total of synthesis of THL-like protein-reactive probes, in which extremely conservative modifications (ie, an alkyne handle) were introduced in the parental THL structure to ...