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- W2000229845 abstract "Antibiotic resistance is a growing problem within the United States, necessitating the need to develop new antimicrobial agents. It has been estimated that within 10 years of an antibiotic entering the market, significant resistance will appear in target bacteria. Exacerbating this problem, many major pharmaceutical companies are not developing new antimicrobial agents, relying on biotech and universities to discover new classes of antibiotics. As a result, only 1% of drugs in clinical trials in 2004 were antibiotics. Because of this, there needs to be a greater push for the design of new antibiotics and antimicrobials to replace obsolete ones as well as development of new, more effective approaches for drug discovery. We have been using a fragment-based approach to identify potential inhibitor building blocks for two bacterial enzymes. Potential building blocks are tested for their ability to inhibit enzyme function and the thermodynamics of binding are investigated by calorimetry. Combinations of these fragments will be combined to develop potential new classes of antibiotics." @default.
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- W2000229845 date "2010-01-01" @default.
- W2000229845 modified "2023-09-28" @default.
- W2000229845 title "Applying Thermodynamics to Fragment-Based Drug Development" @default.
- W2000229845 doi "https://doi.org/10.1016/j.bpj.2009.12.2513" @default.
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