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The time a drug remains bound to its target is an underemphasized factor in drug discovery, according to Peter J. Tonge of the State University of New York, Stony Brook. Tonge discussed this issue during a presentation last week at the American Society for Biochemistry & Molecular Biology annual meeting in Anaheim, Calif. He says his group believes many drugs are effective because they have long residence times on their targets. Researchers have largely ignored this concept and have not usually incorporated it into the drug discovery process, he notes. Tonge’s results suggest that should change. He and his coworkers recently developed compounds that inhibit an enzyme in the bacterium that causes the infectious disease tularemia and found that the compounds’ in vivo activity correlated with the time bound to their target instead of with binding affinity (ACS Chem. Biol. 2009, 4, 221). The researchers also developed a long-residence-time inhibitor of an enzyme in the tuberculosis bacterium (J. Biol. Chem., DOI: 10.1074/jbc.M109.090373) and have since demonstrated its activity in an animal model of tuberculosis. Because such agents overstay their welcome in bacteria, tagged versions might be useful for imaging bacterial populations, Tonge suggests.
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