Work

Correlation of F0F1-ATPase Inhibition and Antiproliferative Activity of Apoptolidin Analogues

Year: 2006

Type: article

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.

Source: Organic Letters

DOI: 10.1021/ol052800q

Authors: Paul A. Wender, Orion D. Jankowski, Kate Longcore, Elie A. Tabet, Haruo Seto, Taijiro Tomikawa

Institutions: Tokyo University of Agriculture, Stanford University

Language: English

Topic: Cell death mechanisms and regulation

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funder: National Cancer Institute