Furin is the first discovered
proprotein convertase member and is present in almost all mammalian cells. Therefore, by regulating the maturation of a wide range of proproteins,
Furin expression and/or activity is involved in various physiological and pathophysiological processes ranging from embryonic development to
carcinogenesis. Since many of these
protein precursors are involved in initiating and maintaining the hallmarks of
cancer,
Furin has been proposed as a potential target for treating several human
cancers. In contrast, other studies have revealed that some types of
cancer do not benefit from
Furin inhibition. Therefore, understanding the heterogeneous functions of
Furin in
cancer will provide important insights into the design of effective strategies targeting
Furin in
cancer treatment. Here, we present recent advances in understanding how
Furin expression and activity are regulated in
cancer cells and their influences on the activity of
Furin substrates in
carcinogenesis. Furthermore, we discuss how
Furin represses tumorigenic properties of several
cancer cells and why
Furin inhibition leads to aggressive phenotypes in other
tumors. Finally, we summarize the clinical applications of
Furin inhibition in treating human
cancers.