Development of an Orally Bioavailable LCK PROTAC Degrader as a Potential Therapeutic Approach to T-Cell Acute Lymphoblastic Leukemia.
J Med Chem
; 67(14): 11868-11884, 2024 Jul 25.
Article
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| MEDLINE
| ID: mdl-38973320
ABSTRACT
Despite significant advances over recent years, the treatment of T cell acute lymphoblastic leukemia (T-ALL) remains challenging. We have recently shown that a subset of T-ALL cases exhibited constitutive activation of the lymphocyte-specific protein tyrosine kinase (LCK) and were consequently responsive to treatments with LCK inhibitors and degraders such as dasatinib and dasatinib-based PROTACs. Here we report the design, synthesis and in vitro/vivo evaluation of SJ45566, a potent and orally bioavailable LCK PROTAC.
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Proteína Tirosina Quinasa p56(lck) Específica de Linfocito
/
Leucemia-Linfoma Linfoblástico de Células T Precursoras
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2024
Tipo del documento:
Article