Dmitrienko, Gary - University of Waterloo

个人简介

Gary Dmitrienko's research involves the application of organic chemical, biochemical and microbiological techniques to the discovery of new treatments for infections caused by bacteria that are resistant to beta-lactam antibiotics such as penicillins, cephalosporins and carbapenems as well as the study of natural antitumour antibiotics. Bioorganic and medicinal chemistry related to antimicrobial and anticancer agents Synthesis of heterocyclic and carbocyclic compounds Mechanistic organic chemistry and biochemistry Natural products chemistry and biochemistry Member of the CIHR Industry-Partnered Collaborative Research grant selection panel, 2012-2015 Member of the Pharmaceutical Sciences operating grant selection panel Canadian Institutes for Health Research, 2007, 2010 1974 PhD, Organic Chemistry, University of Toronto 1970 BSc, Honours Chemistry, University of Toronto

研究领域

Hospital-acquired infections (HAIs) are increasing with growing numbers of susceptible individuals in aging populations. So-called Gram-negative bacteria like Escherichia coli cause many thousands of HAIs each year. The beta-lactamsare the most important antibiotics for HAIs caused by these organisms. Since Gram-negative bacteria have become resistant to most other antibiotics, carbapenems (the most powerful beta-lactams) are now the most important treatment for these infections. Gary Dmitrienko's research focuses on designing, creating and testing molecules that will block carbapenem-resistance mechanisms like NDM-1 and so enable carbapenems to kill resistant Gram-negative bacteria. Natural products with potent antibacterial and anticancer properties are also a major area of interest.

近期论文

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Assay for drug discovery: Synthesis and testing of nitrocefin analogues for use as β-lactamase substrates. Ghavami, A.; Labbé, G.; Brem, J.; Goodfellow, V. J.; Marrone, L., Tanner, C. A.; King, D. T., Lam, M.; Strynadka, N. C.; Pillai, D. R.; Siemann, S.; Spencer, J.; Schofield, C. J.; Dmitrienko, G. I. Anal. Biochem. 2015, 486, 75-7. Arginine-containing peptides as potent inhibitors of VIM-2 metallo-β-lactamase. Rotondo, C. M.; Marrone, L.; Goodfellow, V. J., Ghavami, A.; Labbé, G.; Spencer, J.; Dmitrienko G. I.; Siemann, S. Biochim. Biophys. Acta. 2015, 1850, 2228-38. Prekinamycin and an isosteric-isoelectronic analogue exhibit comparable cytotoxicity towards K562 human leukemia cells, Abbott, G.L.; Wu, X.; Zhao, Z.; Guo, L.; Birman, V.B; Hasinoff, B. B.; Dmitrienko, G.I. Med. Chem. Commun., 2014, 5, 1364-1370. Cyclobutanone Analogues of b-Lactams Revisited: Insights Into Conformational Requirements for Inhibition of Serine- and Metallo-b-Lactamases. Johnson, J. W.; Gretes, M.; Goodfellow, V. J.; Marrone, L.; Heynen, M. L.; Strynadka, N. C. J.; Dmitrienko, G. I. J. Am. Chem. Soc. 2010, 132, 2558–2560. Cyclobutanone Mimics of Penicillins: Effects of Substitution on Conformation and Hemiketal Stability. Johnson, J. W.; Evanoff, D. P.; Savard, M. E.; Lange, G.; Ramadhar, T. R.; Assoud, A.; Taylor, N. J.; Dmitrienko, G. I. J. Org. Chem. 2008, 73, 6970–6982.