Scientific Article
previous document  unige:7726  next document
add to browser collection

Biologically Active Amphotericin B-Calix[4]arene Conjugates

Paquet, Valerie
Carreira, Erick M.
Published in Bioconjugate Chemistry. 2006, vol. 17, no. 6, p. 1460-1463
Abstract In order to provide tools for investigations of amphotericin B ion channels, new conjugates bearing a calix[4]arene scaffold covalently linked to four amphotericin B molecules were synthesized. These macromolecules adopt a cone conformation that mimics the structure of a transmembrane pore. The antifungal activity of the conjugates 3 and 4 was superior or similar to that of native amphotericin B, with minimal inhibitory concentration values of 0.10 and 0.25 microM, respectively. Furthermore, the hemotoxicity of the new conjugates was considerably lower (at least 10 times) than the hemotoxicity of monomeric amphotericin B. Finally, the formation of ion channels in the lipid bilayer by the amphotericin B tetramer was monitored by measuring the K+ efflux from various liposomes.
PMID: 17105224
Full text
Article - document accessible for UNIGE members only Limited access to UNIGE
(ISO format)
PAQUET, Valerie, ZUMBUEHL, Andréas, CARREIRA, Erick M. Biologically Active Amphotericin B-Calix[4]arene Conjugates. In: Bioconjugate Chemistry, 2006, vol. 17, n° 6, p. 1460-1463.

297 hits



Deposited on : 2010-06-21

Export document
Format :
Citation style :