Chapter 10

Drugs That Inhibit Enzymes

Robert E. Smith

Abstract

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.

Total Pages: 342-389 (48)

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