Extracellular proteolysis is an absolute requirement for new blood vessel f
ormation, a process known as angiogenesis. This review will examine the rol
e of the matrix metalloproteinase and plasminogen activator/plasmin systems
during angiogenesis. Extracellular proteolysis has also been implicated in
the generation of molecules with angioregulatory activity. These include,
but are not limited to, angiostatin and endostatin. However, despite an abu
ndance of data on their bioactivity, the molecular mechanisms by which thes
e molecules achieve their effects are unknown. Anti-proteolysis, particular
ly in the context of angiogenesis, has become a key target in therapeutic s
trategies aimed at inhibiting tumor growth and other diseases associated wi
th neovascularization.