Correlation of F0F1-ATPase inhibition and antiproliferative activity of apoptolidin analogues.
Org Lett
; 8(4): 589-92, 2006 Feb 16.
Article
en En
| MEDLINE
| ID: mdl-16468718
ABSTRACT
[structure see text] Apoptolidin (1) exhibits potent and highly selective apoptosis inducing activity against sensitive cancer cell lines and is hypothesized to act by inhibition of mitochondrial F(0)F(1)-ATP synthase. A series of apoptolidin derivatives, including a new intermolecular Diels-Alder adduct, were analyzed for antiproliferative activity in E1A-transformed rat fibroblasts. Potent F(0)F(1)-ATPase inhibition was not a sufficient determinant of antiproliferative activity for several analogues, suggesting the existence of a secondary biological target or more complex mode of action for apoptolidin.
Texto completo:
1
Colección:
01-internacional
Asunto principal:
ATPasas de Translocación de Protón
/
Macrólidos
/
Antineoplásicos
Límite:
Animals
Idioma:
En
Revista:
Org Lett
Asunto de la revista:
BIOQUIMICA
Año:
2006
Tipo del documento:
Article
País de afiliación:
Estados Unidos