19.3 Receptor-Ligand Interractions Flashcards
Two classes of receptors:
Nuclear Hormone receptors: Binds ligands within a cell.
Membrane-bound Receptors: Yeah…
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Nuclear Hormone Receptors are found in what 2 places and they play a role as primarily what?
Are found in the cytosol or inside the nucleus. When in active form, cytosolic NHRs enter the membrane to bind to DNA. NHRs already in nuclear are already attached to DNA, but require a ligand to activate. Both types play a role as transcription factors.
Membrane-bound Receptor Categories
Ion-linked, G Protein coupled, enzyme linked.
Ion linked Receptor Functionality
When a ligand is bound, opens channel for an ionic molecule. Example: Acetylcholine-nicotine receptor.
Cys-loop
Most common ion-channel receptor type. consists of four membrane-bound alpha-helices, and 5 alpha-helix subdomains.
G Protein Coupled Receptor Functionality
Receptors that use heterotrimeric G-proteins to transmit extracellular signals.
7-transmembrane Helix
Most common type of G-protein receptor.
Enzyme-linked Receptors
When substrate binds to receptor, receptor then becomes an enzyme and catalyzes a reaction. Example: Insulin receptor.
Receptor Tyrosine Kinase Functionality
When bound to substrate, causes the receptor to dimerize with another nearby receptor and auto-phosphorylate each other, and then the scaffolding protein.
Agonist, Partial-Agonist and Antagonist
Agonist: binds to receptor, invokes full (or slightly modified) reaction.
Partial-Agonist: Binds to receptor, only invokes partial reaction.
Antagonist: binds to and blocks the receptor.
Types of Agonists and Descriptions
Competitive Agonists: Competes with native ligand for binding site.
Noncompetitive Agonist: Does not compete with native ligand, but lowers the ability of the native ligand to bind to receptor.
Inverse Agonist: Effects the basal level of activity of receptor.
The Langmuir Equation (cannot be used for receptors with allosteric sites)
Used to plot the percentage of bound sites (y) for a given concentration of substrate (x).