Use of Novel Boronic Acid Transition State Inhibitors To Probe Substrate Affinity in SHV-Type Extended-Spectrum β-Lactamases | Zendy

Jodi M. Thomson | Zendy; Fabio Prati | Zendy; Christopher R. Bethel | Zendy; Robert A. Bonomo | Zendy

Open Access

Use of Novel Boronic Acid Transition State Inhibitors To Probe Substrate Affinity in SHV-Type Extended-Spectrum β-Lactamases

Author(s) -

Jodi M. Thomson,

Fabio Prati,

Christopher R. Bethel,

Robert A. Bonomo

Publication year - 2007

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.01293-06

Subject(s) - cefotaxime , ceftazidime , boronic acid , antibiotics , beta lactamase inhibitors , broad spectrum , chemistry , antibacterial agent , microbiology and biotechnology , stereochemistry , biology , biochemistry , bacteria , combinatorial chemistry , pseudomonas aeruginosa , genetics

Boronic acid transition state inhibitors (BATSIs) with R1 side chains of cefotaxime and ceftazidime were assayed against SHV-1, SHV-2, SHV-5, D104K, and D104K G238S beta-lactamases. The D104K variant was the most susceptible to inhibition by the ceftazidime BATSI (Ki, 730+/-80 nM), while the D104K G238S variant was the most susceptible to the cefotaxime BATSI (Ki, 1.1+/-0.2 microM).

The content you want is available to Zendy users.

Already have an account? Click here to sign in.

Having issues? You can contact us here

Accelerating Research