Saidjalolov, Saidbakhrom; Braud, Emmanuelle; Edoo, Zainab; Iannazzo, Laura; Rusconi, Filippo; Riomet, Margaux; Sallustrau, Antoine; Taran, Frederic; Arthur, Michel; Fonvielle, Matthieu; Etheve-Quelquejeu, Melanie published the artcile< Click and Release Chemistry for Activity-Based Purification of 尾-Lactam Targets>, Electric Literature of 112-63-0, the main research area is click release chem beta lactam target screening; Activity-based probe; Antibiotic; Click and release; Iminosydnone; Peptidoglycan.
尾-Lactams, the cornerstone of antibiotherapy, inhibit multiple and partially redundant targets referred to as transpeptidases or penicillin-binding proteins. These enzymes catalyze the essential crosslinking step of the polymerization of cell wall peptidoglycan. The understanding of the mechanisms of action of 尾-lactams and of resistance to these drugs requires the development of reliable methods to characterize their targets. Here, we describe an activity-based purification method of 尾-lactam targets based on click and release chem. We synthesized alkyne-carbapenems with suitable properties with respect to the kinetics of acylation of a model target, the Ldtfm L,D-transpeptidase, the stability of the resulting acylenzyme, and the reactivity of the alkyne for the cycloaddition of an azido probe containing a biotin moiety for affinity purification and a bioorthogonal cleavable linker. The probe provided access to the fluorescent target in a single click and release step.
Chemistry – A European Journal published new progress about Antibiotic resistance. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.
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