Pharmacology
Pharmacology
Core4: Molecular targets of drugs
薬物の分子標的
🎯 High-yield / 要点:Drug targets are not only receptors. Main categories: receptors, enzymes, transporters, ion channels, nucleic acids, microbial targets, non-receptor effects, biologic/cell targets.
Main target classes / 主な標的
| Target | Examples | High-yield point |
|---|---|---|
| Receptors | Intracellular receptors, ligand-gated channels, GPCRs, enzyme-linked receptors | Largest classic pharmacology category |
| Enzymes | COX, ACE, acetylcholinesterase, HMG-CoA reductase | Often inhibited by drugs |
| Transporters | SERT, NET, DAT, intestinal cholesterol transporter | Reuptake/absorption blockade changes concentration |
| Voltage-gated ion channels | Na⁺, K⁺, Ca²⁺ channels | Important in antiarrhythmics and neurologic drugs |
| Nucleic acids | DNA, RNA, siRNA | Common in anticancer/antiviral/targeted therapy |
| Microbial targets | Cell wall, protein synthesis, nucleic acid synthesis | Antibiotic targets |
| Non receptor-mediated | Bile acids, gastric acid, osmotic effects | Effect by binding/neutralizing/physical osmotic action |
| Others | Cytokines, CD20, tubulin | Biologics and cytotoxic drugs |
Receptor subtypes / 受容体標的
- Intracellular receptors:thyroid hormone nuclear receptors; steroid cytoplasmic receptors.
- Ligand-gated ion channels:
- Nicotinic ACh receptor: nicotine, choline esters, skeletal muscle relaxants.
- GABA_A: benzodiazepines, barbiturates, propofol, some anticonvulsants.
- 5-HT3: setrons; NMDA: ketamine; AMPA: topiramate; glycine: strychnine.
- GPCRs:
- Gs:β-adrenergic, D1, glucagon, H₂, prostacyclin.
- Gi:α₂, M₂, D₂, opioid, some serotonin receptors.
- Gq:α₁, M₁/M₃/M₅, AT1, some serotonin receptors.
- Enzyme-linked receptors:tyrosine kinase receptors, TGF-β receptor, guanylate cyclase/ANP.
Remember / 覚え方
- Receptor–Enzyme–Transporter–Channel = core four.
- Antibiotics often target microbial cell wall/protein synthesis/nucleic acid synthesis.
- Antacids/osmotic laxatives work without classic receptors.