Mediaspace scheduled maintenance: Aug 25, 2026 07:00 - 12:00 AM. During this time, videos will be temporarily unavailable. Check status updates.

Lecture

Pharmacodynamics: Ligand-Receptor Binding Kinetics

Description

This lecture covers the quantitative description of ligand-receptor binding at equilibrium, including association and dissociation kinetics, the relationship between ligand concentration, binding, and effect, as well as the mechanisms of agonists, allosteric modulators, and antagonists. It also discusses the measurement and examples of association and dissociation kinetics, the impact of kon and koff rates on drug therapy, and the kinetics of effect appearance and drug washout.

Instructors (2)

Dmitri Firsov

Romain Zufferey

Official source

Related concepts (29)

Ligand (biochemistry)

In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ligare, which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix.

Enzyme kinetics

Enzyme kinetics is the study of the rates of enzyme-catalysed chemical reactions. In enzyme kinetics, the reaction rate is measured and the effects of varying the conditions of the reaction are investigated. Studying an enzyme's kinetics in this way can reveal the catalytic mechanism of this enzyme, its role in metabolism, how its activity is controlled, and how a drug or a modifier (inhibitor or activator) might affect the rate. An enzyme (E) is typically a protein molecule that promotes a reaction of another molecule, its substrate (S).

Ligand binding assay

A ligand binding assay (LBA) is an assay, or an analytic procedure, which relies on the binding of ligand molecules to receptors, antibodies or other macromolecules. A detection method is used to determine the presence and extent of the ligand-receptor complexes formed, and this is usually determined electrochemically or through a fluorescence detection method. This type of analytic test can be used to test for the presence of target molecules in a sample that are known to bind to the receptor.

Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins. They are sometimes called blockers; examples include alpha blockers, beta blockers, and calcium channel blockers. In pharmacology, antagonists have affinity but no efficacy for their cognate receptors, and binding will disrupt the interaction and inhibit the function of an agonist or inverse agonist at receptors.

Ligand-gated ion channel

Ligand-gated ion channels (LICs, LGIC), also commonly referred to as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow ions such as Na+, K+, Ca2+, and/or Cl− to pass through the membrane in response to the binding of a chemical messenger (i.e. a ligand), such as a neurotransmitter. When a presynaptic neuron is excited, it releases a neurotransmitter from vesicles into the synaptic cleft. The neurotransmitter then binds to receptors located on the postsynaptic neuron.

Related lectures (31)

Pharmacodynamics: Ligand Concentration, Binding, and Effect

Explores the relationship between ligand concentration, binding, and effect, focusing on allosteric modulators and types of pharmacological antagonists.

Pharmacodynamics: Ligand-Receptor Interactions and Drug Effects

Explores ligand-receptor interactions, drug effects, modulation mechanisms, and factors influencing drug responses.

Pharmacodynamics: Ligand-Receptor Binding and Drug Effects

Explores ligand-receptor binding, drug effects, efficacy, potency, and biased agonism in pharmacodynamics.

Pharmacodynamics exercises

Covers the analysis of binding measurements and toxin kinetics in pharmacodynamics.

Pharmacodynamics: Quantitative Description of Ligand-Receptor Binding