Title:New Approaches in Sensing and Targeting Bacterial rRNA A-site
VOLUME: 16
Author(s):Preethi Parameswaran, Nihar Ranjan* and S.J.S. Flora*
Affiliation:Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER)- Raebareli, New Transit Campus, Lucknow, Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER)- Raebareli, New Transit Campus, Lucknow, Department of Pharmacology, National Institute of Pharmaceutical Education and Research (NIPER), Raebareli, New Transit Campus, Lucknow
Keywords:A-site, rRNA, FRET, Antimicrobial agents, Drug Discovery.
Abstract:New chemical agents that could combat increasing antibiotic resistance are urgently
needed. In this mini-review, an old but highly relevant RNA sequence which is crucial for the continuation
of bacterial life-cycle is covered. Some of the most significant advances of the last decade
in sensing and targeting the bacterial rRNA A-site: a well-validated binding site of proverbially
known aminoglycoside antibiotics are described. Some of the major advances in direct sensing
of the bacterial decoding side (A-site) are described and also new fluorescent molecules that are
capable of detecting lead compounds through high-throughput assays by displacement of fluorescent
probe molecules are highlighted. Lastly, some of the recently discovered non-aminoglycoside
small molecule binders of bacterial rRNA A-site as a new class of molecules that could provide
future scaffolds and molecules for developing new antibacterial agents have been discussed.
