10 years into the resurgence of covalent drugs.
Future Med Chem
; 13(2): 193-210, 2021 01.
Article
en En
| MEDLINE
| ID: mdl-33275063
ABSTRACT
In the first decade of targeted covalent inhibition, scientists have successfully reversed the previous trend that had impeded the use of covalent inhibition in drug development. Successes in the clinic, mainly in the field of kinase inhibitors, are existing proof that safe covalent inhibitors can be designed and employed to develop effective treatments. The case of KRASG12C covalent inhibitors entering clinical trials in 2019 has been among the hottest topics discussed in drug discovery, raising expectations for the future of the field. In this perspective, an overview of the milestones hit with targeted covalent inhibitors, as well as the promise and the needs of current research, are presented. While recent results have confirmed the potential that was foreseen, many questions remain unexplored in this branch of precision medicine.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Inhibidores de Proteínas Quinasas
Límite:
Humans
País/Región como asunto:
America do norte
Idioma:
En
Revista:
Future Med Chem
Año:
2021
Tipo del documento:
Article
País de afiliación:
Reino Unido