Lim Taehyeong, Ham So-Young, Nam SangJin, Kim Myoungsun, Lee Ki Yong, Park Hee-Deung, Byun Youngjoo
College of Pharmacy, Korea University, Sejong 30019, Korea.
School of Civil, Environmental and Architectural Engineering, Korea University, Seoul 02841, Korea.
Antibiotics (Basel). 2022 Feb 19;11(2):274. doi: 10.3390/antibiotics11020274.
(. ) is an opportunistic gram-negative pathogen that can cause various infections, particularly in patients with compromised host defenses. . forms biofilms and produces virulence factors through quorum sensing (QS) network, resulting in resistance to antibiotics. RhlI/RhlR, one of key QS systems in . , is considered an attractive target for inhibiting biofilm formation and attenuating virulence factors. Several recent studies examined small molecules targeting the RhlI/RhlR system and their in vitro and in vivo biological activities. In this review, RhlR-targeted modulators, including agonists and antagonists, are discussed with particular focus on structure-activity relationship studies and outlook for next-generation anti-biofilm agents.
（某菌）是一种机会性革兰氏阴性病原体，可引起各种感染，尤其是在宿主防御功能受损的患者中。（某菌）形成生物膜并通过群体感应（QS）网络产生毒力因子，从而导致对抗生素产生耐药性。RhlI/RhlR是（某菌）关键的QS系统之一，被认为是抑制生物膜形成和减弱毒力因子的一个有吸引力的靶点。最近的几项研究检测了靶向RhlI/RhlR系统的小分子及其体外和体内生物学活性。在这篇综述中，将讨论靶向RhlR的调节剂，包括激动剂和拮抗剂，特别关注构效关系研究以及下一代抗生物膜药物的前景。
