Drug Targets

• Four major protein targets for drugs

  1. Receptors

  2. Carrier molecules (Transporters)

  3. Ion channels (bind or move target molecules)

  4. Enzymes (convert substrates into products)
• Receptors are complex macromolecules to which endogenous mediators (eg. hormones, neurotransmitters) bind and initiate changes in cellular function

  • Most receptors are embedded in cell membranes

  • All receptors that exist in the organism have physiologic roles, and no receptor has been specifically ‘allocated’ for drugs
• Ligand binding to a receptor initiates signals inside the cell