Antibody drug conjugates with hydroxamic acid cargos for histone deacetylase (HDAC) inhibition.
Chem Commun (Camb)
; 57(7): 867-870, 2021 Jan 28.
Article
en En
| MEDLINE
| ID: mdl-33433550
ABSTRACT
Antitumor hydroxamates SAHA and Dacinostat have been linked to cetuximab and trastuzumab through a non-cleavable linker based on the p-mercaptobenzyl alcohol structure. These antibody drug conjugates (ADCs) were able to inhibit HDAC in several tumour cell lines. The cetuximab based ADCs block human lung adenocarcinoma cell proliferation, demonstrating that bioconjugation with antibodies is a suitable approach for targeted therapy based on hydroxamic acid-containing drugs. This work also shows that ADC-based delivery might be used to overcome the classical pharmacokinetic problems of hydroxamic acids.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inmunoconjugados
/
Inhibidores de Histona Desacetilasas
/
Histona Desacetilasas
/
Ácidos Hidroxámicos
Límite:
Humans
Idioma:
En
Revista:
Chem Commun (Camb)
Asunto de la revista:
QUIMICA
Año:
2021
Tipo del documento:
Article
País de afiliación:
Italia