This paper reviews the current status of our understanding of azole an
tifungal resistance mechanisms at the molecular level and explores the
ir implications. Extensive biochemical studies have highlighted a sign
ificant diversity in mechanisms conferring resistance to azoles, which
include alterations in sterol biosynthesis, target site, uptake and e
fflux. In stark contrast, few examples document the molecular basis of
azole resistance. Those that do refer almost exclusively to mechanism
s in laboratory mutants, with the exception of the role of multi-drug
resistance proteins in clinical isolates of Candida albicans. It is cl
ear that the technologies required to examine and define azole resista
nce mechanisms at the molecular level exist, but research appears dist
inctly lacking in this most important area.