ENZIM SEBAGAI TARGET AKSI OBAT

ENZIM

Enzim merupakan suatu ___________ yang berfungsi sebagai __________ proses-proses kimia atau biokimia dalam tubuh

Contoh-contoh (1)

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 acidDihydropteroate synthetase is a required

enzyme in the bacterial synthesis of folic acidSulfa drugs (eg. sulfanilamide, 1935) inhibit

dihydropteroate synthetase and are bacteriostatic

5

Ex: Menghambat metabolisme sel mikroba (bakteriostatik)

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

6

Enzyme Inhibitors as Drugs (2) 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

RT Structure

Enzim COX (3)

Neurotransmiter dan enzim (4) Contoh neurotransmiter : Asetilkolin

(Ach), Gaba, serotonin, epinefrin

(a) asetilkolin

(b) GABA

Chemical deficiencies can be corrected by inhibiting an enzyme that uses the chemical as a substrate

1. Seizures can be caused by insufficient γ-aminobutyric acid (GABA)

2. GABA is degraded by GABA-aminotransferase enzyme

3. GABA-aminotransferase inhibitors are anticonvulsant

ENZIM GABA-TRANSAMINASE

XO (5)Chemical excess can be corrected by

inhibiting an enzyme that produces the molecule

1. Gout results from excess uric acid2. Xanthine oxidase converts xanthine to

uric acid3. Inhibitors of xanthine oxidase reduce

levels of uric acid