Strategies for designing proteolysis targeting chimaeras (PROTACs).
Med Res Rev
; 42(3): 1280-1342, 2022 05.
Article
en En
| MEDLINE
| ID: mdl-35001407
ABSTRACT
Proteolysis targeting chimaeras (PROTACs) is a cutting edge and rapidly growing technique for new drug discovery and development. Currently, the largest challenge in the molecular design and drug development of PROTACs is efficient identification of potent and drug-like degraders. This review aims to comprehensively summarize and analyse state-of-the-art methods and strategies in the design of PROTACs. We provide a detailed illustration of the general principles and tactics for designing potent PROTACs, highlight representative case studies, and discuss the advantages and limitations of these strategies. Particularly, structure-based rational PROTAC design and emerging new types of PROTACs (e.g., homo-PROTACs, multitargeting PROTACs, photo-control PROTACs and PROTAC-based conjugates) will be focused on.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Descubrimiento de Drogas
Límite:
Humans
Idioma:
En
Año:
2022
Tipo del documento:
Article