Assays for beta-lactamase activity and inhibition

The ability, either innate or acquired, to produce beta-lactamases, Enzymes capable of hydrolyzing the endocyclic peptide bond in Beta-lactam Antibiotics, would appear to be a primary contributor to the ever-increasing incidences of resistance to this class of Antibiotics. To date, four distinct classes, A, B, C, and D, of beta-lactamases have been identified. Of these, Enzymes in classes A, C, and D utilize a serine residue as a nucleophile in their catalytic mechanism while class B members are Zn2+-dependent for their function. Efforts have been and still continue to be made toward the development of potent inhibitors of these Enzymes as a means to ensure the efficacy of Beta-lactam Antibiotics in clinical medicine. This chapter concerns procedures for the evaluation of the catalytic activity of beta-lactamases as a means to screen compounds for their inhibitory potency.