Drug affinity responsive target stability (DARTS) accelerated small molecules target discovery: Principles and application.
Biochem Pharmacol
; 194: 114798, 2021 12.
Article
en En
| MEDLINE
| ID: mdl-34678227
ABSTRACT
Drug affinity responsive target stability (DARTS) is a novel target discovery approach and is particularly adept at screening small molecule (SM) targets without requiring any structural modifications. The DARTS method is capable of revealing drug-target interactions from cells or tissues by tracking changes in the stability of proteins acting as receptors of bioactive SMs. Due to its simple operation and high efficiency, the DARTS method has been applied to uncover the drug-action mechanism. This review summarized analytical principles, protocols, validation approaches, applications, and challenges involved in the DARTS method. Due to the innate advantages of the DARTS method, it is expected to be a powerful tool to accelerate SM target discovery, especially for bioactive natural products with unknown mechanisms.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Sistemas de Liberación de Medicamentos
/
Bibliotecas de Moléculas Pequeñas
/
Descubrimiento de Drogas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Biochem Pharmacol
Año:
2021
Tipo del documento:
Article