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Cell Receptors

Chemistry of recoptor binding, modulators, agonist and antagonists

Most receptors are located in... the cell membrane
Receptors are activated by... Chemical messengers
Chemical messengers include _____ and ______ neurotransmitters and hormones
Binding of messenger to receptor results in _______ _______ Signal transduction
Drug that mimics natural messenger is an _____ agonist
Agonist should bind and leave quickly or slowly? quickly
Drug that blocks natural messenger is an _____ antagonist
Antagonists alter induced fit due to _____ and/or _____ binding groups stronger and/or more binding groups
Agonist must have correct ____ , ______ and ____ _____ in order to work correct shape , positioning and binding groups
Enantiomers usually have ______ biological properties different
Agonists usually have _____ of interactions as natural messenger same #
Groups that block access to binding site are called ______ or ______ steric blocks or steric shields
Agents which bind to allosteric binding site rather than the messenger binding site allosteric modulators
Allosteric modulators _______ receptor activity enhance
Ex. of Allosteric modulator benzodiazepines
Benzodiazepines target allosteric site of GABAa receptor
Reversible antagonist binds _____ to receptor and produces different ____ ___ reversibly , induced fit
Does antagonist undergo rxn with receptor? no rxn
Level of antagonism depends on _____ of binding and _______ strength and [antagonist]
For reversible antagonist: increasing [messenger].... lowers antagonism
Irreversible antagonists bind _____ to receptor by form ______ bonds irreversibly , covalent
For irreversible antagonists: increasing [messenger]... does not reverse antagonism
Allosteric antagonist bind ______ to _______ site of receptor reversibly , allosteric
Alloseric antagonist work by.... altering shape of receptor to block messenger action
For Allosteric antagonists: increasing [messenger]... does not reverse antagonism
How does Antagonism by Umbrella effect work? Antagonist binds to neighboring binding site and overlaps/covers messenger binding site
______ ______ binds but does not produce maximum effect Partial agonist
Partial agonists act as _____ to one receptor subtype and ______ to different subtype agonist , antagonist
Define Inherent activity any activity present in the absence of a chemical messenger
Inverse agonist blocks ______ ______ of receptor inherent activity
Inverse agonist create equilibrium between ______ activity and _______ inherent activity and inactivity
Adding agonist pushed receptor toward _____ form active
Adding antagonist pushes receptor toward ____ form inactive
Adding partial agonist pushes receptor toward ______ between forms equilibrium
Receptors become ____ after long-term exposure to agonist desensitized
Prolonged binding of agonist leads to ______ of receptor phosphorylation
Phosphorylation _______ receptor until agonist leaves deactivates
Receptors become ______ after long-term exposure to antagonist sensitized
To compensate for antagonist-blocked receptors, cell.... synthesizes new receptors
Synthesis of new receptors makes cell more sensitive to _______ natural messenger
Long-term exposure to agonist can lead to ______ and ______ tolerance and dependence
Tolerance results in need to.... increase dosage of antagonist
Dependence results from ______ symptoms when antagonist is taken away withdrawal
Estradiol binding to estrogen receptor results in _______ and exposure of _____ dimerization , AF-2 regions
_______ binds to AF-2 regions of estrogen receptor in order to activate response Coactivator
Raloxifene is an estrogen receptor ______ and ______ agent antagonist and anti-cancer
Raloxifene works by preventing ______ so _____ regions are not exposed and coactivator doesn't bind dimerization , AF-2
Tamoxifen is an estrogen receptor ______ antagonist
Created by: kristin_leann