An Exceptionally Potent Inhibitor of Human CD73.
Biochemistry
; 58(31): 3331-3334, 2019 08 06.
Article
en En
| MEDLINE
| ID: mdl-31334635
ABSTRACT
We recently reported the initiation of a Phase I clinical trial with AB680, a potent human CD73 inhibitor, being developed for the treatment of solid tumors (NCT03677973). We undertook a detailed kinetic analysis of the interaction between human CD73 and AB680 to determine the mode of inhibition. We found AB680 to be a reversible, slow-onset competitive inhibitor of human CD73 with a Ki of 5 pM. Clinical candidates of this potency are uncommon and deserve special consideration during lead optimization.
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
5'-Nucleotidasa
/
Inhibidores Enzimáticos
Límite:
Humans
Idioma:
En
Revista:
Biochemistry
Año:
2019
Tipo del documento:
Article
País de afiliación:
Estados Unidos