Discovery and characterization of novel TRPML1 agonists.
Bioorg Med Chem Lett
; 98: 129595, 2024 Jan 15.
Article
en En
| MEDLINE
| ID: mdl-38141860
ABSTRACT
Screening a library of >100,000 compounds identified the substituted tetrazole compound 1 as a selective TRPML1 agonist. Both enantiomers of compound 1 were separated and profiled in vitro and in vivo. Their selectivity, ready availability and CNS penetration should enable them to serve as the tool compounds of choice in future TRPML1 channel activation studies. SAR studies on conformationally locked macrocyclic analogs further improved the TRPML1 agonist potency while retaining the selectivity.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Tetrazoles
/
Canales de Potencial de Receptor Transitorio
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2024
Tipo del documento:
Article