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Protease Inhibitors

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 effective treatments.






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