There are many important drugs that inhibit enzymes. They include drugs to
prevent heart attacks, pain relievers, antibiotics to cure bacterial infections,
chemotherapeutic drugs to help cure cancer, anti-malarial drugs, sleeping pills, medicines
for high blood pressure, and drugs to treat diabetes, asthma, HIV, seasonal flu, fungus
infections, parasitic worm infections and osteoporosis. Enzymes that are inhibited by FDAapproved
drugs include acetylcholine esterase, AChE; cyclooxygenase; enzymes that
catalyze a key reaction in the synthesis of bacterial cell walls; the protein-RNA complex of
the 30S subunit of the bacterial ribosome; bacterial DNA-gyrase; topoisomerase; bacterial
tetrahydrofolate reductase; a reductase that catalyzes the synthesis of mycolic acids in
Mycobacterium tuberculosis; angiotensin-converting enzyme, or ACE; renin; type 5
phosphodiesterase (PDE-5); farnesyl pyrophosphate synthase; inosine-5’-monophosphate
dehydrogenase (IMPDH); calcineurin; HIV reverse transcriptase; fungal enzymes;
pyruvate-ferridoxin oxidoreductase; aromatase; topoisomerase; BCR-ABL tyrosine kinase;
the proteasome,; histone deacetylase,; thymidylate synthase; viral neuraminidase, viral
thymidine kinase; L-amino acid decarboxylase; xanthine oxidase; and dipeptidyl peptidase-
4 (DPP-4). Drugs are being developed that bind to allosteric sites on enzymes, partially
inhibiting them and causing fewer side effects than drugs already developed that target
active sites.
Keywords: Enzymes, acetylcholine esterase, Mycobacterium tuberculosis, HIV.
