Biochemical Characterization of QPX7728, a New Ultrabroad-Spectrum Beta-Lactamase Inhibitor of Serine and Metallo-Beta-Lactamases-Reference-Cited by-同舟云学术

Biochemical Characterization of QPX7728, a New Ultrabroad-Spectrum Beta-Lactamase Inhibitor of Serine and Metallo-Beta-Lactamases

Published:2020-05-21 Issue:6 Volume:64 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Tsivkovski Ruslan¹,Totrov Maxim²,Lomovskaya Olga¹

Affiliation:

1. Qpex Biopharma Inc., San Diego, California, USA

2. Molsoft L.L.C., San Diego, California, USA

Abstract

QPX7728 is a new ultrabroad-spectrum inhibitor of serine and metallo-beta-lactamases (MBLs) from a class of cyclic boronates that gave rise to vaborbactam. The spectrum and mechanism of beta-lactamase inhibition by QPX7728 were assessed using purified enzymes from all molecular classes. QPX7728 inhibits class A extended-spectrum beta-lactamases (ESBLs) (50% inhibitory concentration [IC 50 ] range, 1 to 3 nM) and carbapenemases such as KPC (IC 50 , 2.9 ± 0.

Funder

Biomedical Advanced Research and Development Authority

HHS | Biomedical Advanced Research and Development Authority

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.00130-20

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