The importance of drug-target residence time.
2009; National Institutes of Health; Volume: 12; Issue: 4 Linguagem: Inglês
Autores
Rumin Zhang, Frederick J. Monsma,
Tópico(s)Receptor Mechanisms and Signaling
ResumoThe importance of kinetics in drug-target interactions, and particularly the residence time of a drug with its target, is increasingly recognized to play a pivotal role in determining both the efficacy and toxicity of a drug. Drug residence time can often be demonstrated to be a key differentiating factor between drugs that act upon a common target. Drug-target residence time can result in either favorable or unfavorable outcomes, and the use of such information could lead to the more efficient design of best-in-class drugs. This review highlights several key concepts and observations related to drug-target residence time, and suggests the use of a kinetics-perceptive and energetics-informed approach to address the challenges facing current drug discovery efforts.
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