(-)-Englerinâ
A is a potent and selective activator of TRPC4 and TRPC5 calcium channels.
Angew Chem Int Ed Engl
; 54(12): 3787-91, 2015 Mar 16.
Article
en En
| MEDLINE
| ID: mdl-25707820
ABSTRACT
Current therapies for common types of cancer such as renal cell cancer are often ineffective and unspecific, and novel pharmacological targets and approaches are in high demand. Here we show the unexpected possibility for the rapid and selective killing of renal cancer cells through activation of calcium-permeable nonselective transient receptor potential canonical (TRPC) calcium channels by the sesquiterpene (-)-englerinâ
A. This compound was found to be a highly efficient, fast-acting, potent, selective, and direct stimulator of TRPC4 and TRPC5 channels. TRPC4/5 activation through a high-affinity extracellular (-)-englerinâ
A binding site may open up novel opportunities for drug discovery aimed at renal cancer.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Sesquiterpenos de Guayano
/
Canales Catiónicos TRPC
Límite:
Humans
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Año:
2015
Tipo del documento:
Article