Use of novel boronic acid transition state inhibitors to probe substrate affinity in SHV-type extended-spectrum beta-lactamases.

نویسندگان

  • Jodi M Thomson
  • Fabio Prati
  • Christopher R Bethel
  • Robert A Bonomo
چکیده

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).

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عنوان ژورنال:
  • Antimicrobial agents and chemotherapy

دوره 51 4  شماره 

صفحات  -

تاریخ انتشار 2007