Sarah Barelier, Romain Avellan, Giri Raj Gnawali, Patrick Fourquet, Véronique Roig-Zamboni, Isabelle Poncin, Vanessa Point, Yves Bourne, Stéphane Audebert, Luc Camoin, Christopher D Spilling, Stéphane Canaan, Jean-François Cavalier, Gerlind Sulzenbacher
A hallmark of Mycobacterium tuberculosis (M. tb), the etiologic agent of tuberculosis, is its ability to metabolize host-derived lipids. However, the enzymes and mechanisms underlying such metabolism are still largely unknown. We previously reported that the Cyclophostin & Cyclipostins (CyC) analogs, a new family of potent antimycobacterial molecules, react specifically and covalently with (Ser/Cys)-based enzymes mostly involved in bacterial lipid metabolism. Here, we report the synthesis of new CyC alkyne-containing inhibitors (CyCyne ) and their use for the direct fishing of target proteins in M...
October 5, 2022: FEBS Journal