CC2 – Drug-target interaction

CC2. Drug–target interaction describes the different ways a drug interacts with a target to produce a biological effect.

2.1. A drug’s ability to interact with a drug target is determined by the intermolecular forces and steric match between drug and binding site.

2.2. Drugs can bind to their targets reversibly or irreversibly depending on the type of bonds formed.

2.3. Competitive interactions occur at the active/orthosteric site while allosteric interactions occur elsewhere on the drug target.

2.4. Agonists are endogenous or exogenous molecules that have affinity for and efficacy at a receptor to elicit a biological response.

2.5. Antagonists are molecules that have affinity for a receptor to limit the effect of agonists but lack intrinsic efficacy.

2.6. Enzyme inhibitors are molecules with affinity for an enzyme to limit their enzymatic activity.

2.7. Transporter inhibitors are molecules that have affinity for transporter proteins to limit the transport of ions, electrolytes or molecules across membranes.

2.8. Biological therapeutics (biologics) are compounds derived from living organisms that target specific mediators of biological responses (e.g., inflammatory and immunological).