Pozzi Cecilia
Department of Biotechnology, Chemistry and Pharmacy-Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.
Antibiotics (Basel). 2020 May 28;9(6):290. doi: 10.3390/antibiotics9060290.
In bacteria, a major resistance mechanism to β-lactam antibiotics is the production of one or more β-lactamase enzymes. β-Lactamases belong to two structurally and mechanistically unrelated families of enzymes, serine-β-lactamases (SBLs; classes A, C, and D) and metallo-β-lactamases (MBLs; class B). The interest in discovering novel inhibitors has recently renewed to counter the threat from newer β-lactamases, such as the extended spectrum β-lactamases (ESBLs) and carbapenemases, that are not inhibited by classical SBL inhibitors. Although resistance development is an ordinary evolutionary process, it has been significantly accelerated by the widespread and uncontrolled misuse of antibiotics and, nowadays, it represents one of the most relevant threats for human health.This Special Issue includes full research articles, brief reports and reviews focused on the targeting of b-lactamases to fight bacterial drug resistance.[...].
在细菌中,对β-内酰胺抗生素的主要耐药机制是产生一种或多种β-内酰胺酶。β-内酰胺酶属于两个结构和作用机制不相关的酶家族,即丝氨酸-β-内酰胺酶(SBLs;A、C和D类)和金属-β-内酰胺酶(MBLs;B类)。最近,人们重新燃起了发现新型抑制剂的兴趣,以应对新型β-内酰胺酶带来的威胁,例如超广谱β-内酰胺酶(ESBLs)和碳青霉烯酶,这些酶不受经典SBL抑制剂的抑制。尽管耐药性的产生是一个正常的进化过程,但抗生素的广泛和无节制滥用已使其显著加速,如今,它已成为对人类健康最严重的威胁之一。本期特刊包括专注于靶向β-内酰胺酶以对抗细菌耐药性的完整研究论文、简短报告和综述。[...]