A molecule that can prevent
the function of a protease is known as an inhibitor. Many inhibitors
directly interfere with the function of a protease by binding in its
active site crevice, denying access by normal peptide substrates. Some
naturally occurring inhibitors (particularly large proteins) bind to
the outside surface of a protease and either mask the active site or
influence the shape of the protease so that peptide substrates cannot
enter the active site.
Serpin - protease complex.
Inhibitors can block the
regulatory functions of proteases in conception, birth, developmental
biology, digestion, growth, maturation, ageing, diseases and death of
all organisms. Genetic or environmental conditions can result in an
over- or under- abundance of proteases or of their natural
inhibitors/activators, leading to abnormal physiology and disease.
Renin involved in hypertension.
Small molecule inhibitors of
proteases are very effective medicines, and are currently available in
man for treating HIV/AIDS, stroke and coronary infarction; and high
blood pressure. Other protease inhibitors are being developed to treat
parasitic, fungal, and viral infections. Diseases of the aged, like
Alzheimer's disease, arthritis, osteoporosis, inflammatory syndromes,
cancers, diabetes, blood pressure and heart diseases are all associated
with proteases, and inhibitors of the relevant proteases promise to be