Enzymes are the catalysts of biochemical reactions in the cell.
Numerous drugs are enzyme inhibitors.
Prominent enzymes as drug targets:
- HIV protease - essential for HIV replication.
Its inhibitor has been able to control AIDS.
- Angiotensin converting enzyme (ACE)
- promotes contraction of
blood vessels. Its inhibitors have been widely used to treat high blood pressure and
congestive heart failure.
- HMG-CoA reductase - essential for the synthesis of
cholesterol. Its inhibitors (such as statins) can reduce the cholesterol level.
- cGMP phosphodiesterase - catalyzes
the conversion of cGMP into GMP. It is the target of the well known
drug for treating impotence, Viagra.
- Calcineurin - a
phosphatase that plays an important role in immune responses. It is the
target of the immunosuppressive drugs FK506 and cyclosporin A.
Review Articles:
Matrix
Metalloproteinases and Tissue Inhibitors of Metalloproteinases - Circulation
Research, 2003.
RNase P: Variations
and Uses - J. Biol. Chem., 2002.
Matrix
metalloproteinases: effectors of development and normal physiology - Genes and Development,
2000.
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