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.