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Lecture

Receptor-Ligand Interaction: Quantification and Mechanisms

In course

CH-411: Cellular signalling

Presentation of selected signalling pathways with emphasis on both the mechanism of action of the molecules involved, molecular interactions and the role of their spatio-temporal organization within the cell, considering cellular dimensions and conditions. ...

Description

This lecture covers methods to quantify receptor-ligand interactions, including rapid filtration and ligand-binding assays with competition. It discusses the impact of reversible inhibitors on binding sites, equilibrium binding, and the effects of mutations on binding and activation. The presentation also delves into ligand-gated ion channels, isothermal titration calorimetry, and the relationship between ligand binding and cellular effects. The instructor explores the Hill equation, cooperativity, and further reading on drug-target residence time. The lecture concludes with a preview of next week's topic on molecular interactions.

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Instructor

Rudolf Hovius

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Related concepts (32)

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.

Receptor (biochemistry)

In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and produce physiological responses such as change in the electrical activity of a cell. For example, GABA, an inhibitory neurotransmitter inhibits electrical activity of neurons by binding to GABA_A 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.

Quantifier (logic)

In logic, a quantifier is an operator that specifies how many individuals in the domain of discourse satisfy an open formula. For instance, the universal quantifier in the first order formula expresses that everything in the domain satisfies the property denoted by . On the other hand, the existential quantifier in the formula expresses that there exists something in the domain which satisfies that property. A formula where a quantifier takes widest scope is called a quantified formula.

Universal quantification

In mathematical logic, a universal quantification is a type of quantifier, a logical constant which is interpreted as "given any", "for all", or "for any". It expresses that a predicate can be satisfied by every member of a domain of discourse. In other words, it is the predication of a property or relation to every member of the domain. It asserts that a predicate within the scope of a universal quantifier is true of every value of a predicate variable.

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