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ID: ALA5226340

Journal: J Med Chem

Title: Chemical Biology of Sortase A Inhibition: A Gateway to Anti-infective Therapeutic Agents.

Authors: Sapra R, Rajora AK, Kumar P, Maurya GP, Pant N, Haridas V.

Abstract: Staphylococcus aureus is the leading cause of hospital-acquired infections. The enzyme sortase A, present on the cell surface of S. aureus, plays a key role in bacterial virulence without affecting the bacterial viability. Inhibition of sortase A activity offers a powerful but clinically less explored therapeutic strategy, as it offers the possibility of not inducing any selective pressure on the bacteria to evolve drug-resistant strains. In this Perspective, we offer a chemical space narrative for the design of sortase A inhibitors, as delineated into three broad domains: peptidomimetics, natural products, and synthetic small molecules. This provides immense opportunities for medicinal chemists to alleviate the ever-growing crisis of antibiotic resistance.

CiteXplore: 34516107

DOI: 10.1021/acs.jmedchem.1c00386