Semantic Scholar Open Access 2018 131 sitasi

The Continuing Challenge of Metallo-β-Lactamase Inhibition: Mechanism Matters.

Lincheng Ju Zishuo Cheng W. Fast R. Bonomo M. Crowder

Lihat Sumber DOI

Abstrak

Metallo-β-lactamases (MBLs) are a significant clinical problem because they hydrolyze and inactivate nearly all β-lactam-containing antibiotics. These 'lifesaving drugs' constitute >50% of the available contemporary antibiotic arsenal. Despite the global spread of MBLs, MBL inhibitors have not yet appeared in clinical trials. Most MBL inhibitors target active site zinc ions and vary in mechanism from ternary complex formation to metal ion stripping. Importantly, differences in mechanism can impact pharmacology in terms of reversibility, target selectivity, and structure-activity relationship interpretation. This review surveys the mechanisms of MBL inhibitors and describes methods that determine the mechanism of inhibition to guide development of future therapeutics.

Topik & Kata Kunci

Medicine Chemistry

Penulis (5)

Lincheng Ju

Zishuo Cheng

W. Fast

R. Bonomo

M. Crowder

Format Sitasi

APA MLA BibTeX

Ju, L., Cheng, Z., Fast, W., Bonomo, R., Crowder, M. (2018). The Continuing Challenge of Metallo-β-Lactamase Inhibition: Mechanism Matters.. https://doi.org/10.1016/j.tips.2018.03.007

Akses Cepat

Lihat di Sumber doi.org/10.1016/j.tips.2018.03.007

Informasi Jurnal

Tahun Terbit: 2018
Bahasa: en
Total Sitasi: 131×
Sumber Database: Semantic Scholar
DOI: 10.1016/j.tips.2018.03.007
Akses: Open Access ✓