The importance of drug-target residence time.
Curr Opin Drug Discov Devel
; 12(4): 488-96, 2009 Jul.
Article
en En
| MEDLINE
| ID: mdl-19562645
ABSTRACT
The 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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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Farmacocinética
/
Preparaciones Farmacéuticas
/
Sistemas de Liberación de Medicamentos
/
Descubrimiento de Drogas
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
Curr Opin Drug Discov Devel
Asunto de la revista:
FARMACOLOGIA
/
TERAPIA POR MEDICAMENTOS
Año:
2009
Tipo del documento:
Article
País de afiliación:
Estados Unidos