Buynak John D
Department of Chemistry, Southern Methodist University, Dallas, TX 75275-0314, USA.
Biochem Pharmacol. 2006 Mar 30;71(7):930-40. doi: 10.1016/j.bcp.2005.11.012. Epub 2005 Dec 13.
Microbial resistance necessitates the search for new targets and new antibiotics. However, it is likely that resistance problems will eventually threaten these new products and it may, therefore, be instructive to review the successful employment of beta-lactam antibiotic/beta-lactamase inhibitor combinations to combat penicillin resistance. These combination drugs have proven successful for more than two decades, with inhibitor resistance still being relatively rare. The beta-lactamase inhibitors are mechanism-based irreversible inactivators. The ability of the inhibitors to avoid resistance may be due to the structural similarities between the substrate and inhibitor.
微生物耐药性使得寻找新靶点和新抗生素成为必要。然而，耐药性问题最终可能会威胁到这些新产品，因此，回顾β-内酰胺抗生素/β-内酰胺酶抑制剂联合用药对抗青霉素耐药性的成功应用可能具有指导意义。这些联合用药已成功应用二十多年，抑制剂耐药性仍然相对少见。β-内酰胺酶抑制剂是基于机制的不可逆失活剂。抑制剂避免产生耐药性的能力可能归因于底物和抑制剂之间的结构相似性。
