Biologie cellulaire : recherche et thérapie

Molecular targets of b-lactams-beyond the usual suspects

Monika I Konaklieva

b-Lactams have historically been viewed as a class of antimicrobials. However, this paradigm is shi ing towards a focus on their ability to function as inhibitors of bacterial enzymes, particularly those involved in broad-spectrum b-lactam resistance, i.e., extended spectrum b-lactamases (ESBL).  is shi in focus is the result of the recognition of the b-lactam’s ability to acylate enzymes, the majority of which have serine as nucleophile in the active site.In addition to being inhibitors of bacterial enzymes, b-lactams also inhibit viral and mammalian serine enzymes demonstrating inter-kingdom activity.  e focus of this presentation is on the evaluation of the potential of b-lactam antibiotics as inhibitors of the serine enzymes of both prokaryotic and eukaryotic origin, with speci­ c focus on the structure-function relationship of b-lactams as antimicrobial and antineoplastic agents.