Using Novel Boronic Acid Transition State Inhibitors to Probe Substrate
نویسندگان
چکیده
3 Running Title: Boronic Acid Inhibitors and SHV 4 5 Jodi M. Thomson, Fabio Prati, Christopher R. Bethel, and Robert A. Bonomo* 6 7 8 Department of Pharmacology, Case Western Reserve University School of Medicine, 9 Cleveland, Ohio; Department of Chemistry, University of Modena, Modena, Italy; 10 Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, OH 11 12 13 14 15 *Correspondence 16 Robert A. Bonomo 17 Louis Stokes Cleveland Veterans Affairs Medical Center 18 10701 East Blvd., Cleveland, Ohio 44106 19 Phone (216) 791-3800x4399 20 Fax: 216-231-3482 21 E-mail: [email protected] 22 23 AC CE PT ED Copyright © 2007, American Society for Microbiology and/or the Listed Authors/Institutions. All Rights Reserved. Antimicrob. Agents Chemother. doi:10.1128/AAC.01293-06 AAC Accepts, published online ahead of print on 12 January 2007
منابع مشابه
Use of novel boronic acid transition state inhibitors to probe substrate affinity in SHV-type extended-spectrum beta-lactamases.
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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