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Inhibition of biochemical pathways unique to a pathogen (bacteria, virus or parasite) can reduce growth or kill the pathogen Bacteria, but not humans, synthesize folic acid Dihydropteroate synthetase is a required enzyme in the bacterial synthesis of folic acid Sulfa drugs (eg. sulfanilamide, 1935) inhibit dihydropteroate synthetase and are bacteriostatic
Sulfonamid, trimetoprim-
sulfametoksazol (kotrimoksazol), PAS, etambutol, sulfon (dapson) Infeksi saluran kemih, saluran nafas & saluran cerna
Tetrahidrofolat penting untuk reaksi transfer 1 atom C pada pembentukan basa purin, asam amino metionin & glisin
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Example 1: Human Immunodeficiency Virus (HIV) Reverse Transcriptase (RT) RT catalyzes the production of viral DNA from the viral RNA template Both competetive and noncompetetive inhibitors are known Both competetive and noncompetetive inhibitors are used clinically
Chemical deficiencies can be corrected by inhibiting an enzyme that uses the chemical as a substrate 1. Seizures can be caused by insufficient aminobutyric acid (GABA) 2. GABA is degraded by GABAaminotransferase enzyme 3. GABA-aminotransferase inhibitors are anticonvulsant
Chemical excess can be corrected by inhibiting an enzyme that produces the molecule 1. Gout results from excess uric acid 2. Xanthine oxidase converts xanthine to uric acid 3. Inhibitors of xanthine oxidase reduce levels of uric acid