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Receptors
Detection of extracellular signals. Dr. Spencer
33
Biochemistry
Graduate
12/16/2010

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Term
ligand
Definition
Molecule that binds to a protein (Ex. first messenger binding to a receptor)
Term
Agonist
Definition
Ligand that activates function (signal Transduction)
Term
Antagonist
Definition
Ligand that prevents function (signal Transduction)
Term
Effector
Definition
Intracellular protein that responds to an activated receptor that generates second messengers.
Term
coupler
Definition
intracellular protein that transmits the signal of an activated receptor to an effector protein
Term
Adaptor
Definition
Intracellular protein that lacks intrinsic enzymatic activity but contains several domains that mediate protein-protein interaction
Term
How do Receptors Display specificity?
Definition
By detecting signaling molecules the cell wants to detect
Term
2 types of molecular switches
Definition
G-Protein Cycle & Protein Phosphorylation
Term
4 types of Cell-surface receptors
Definition
Ligand gated ion channel
-enzyme linked
-cytokin
-G-protien coupled
Term
Ligand-Gated-ion channel action
Definition
Binding of ligand changes ion permeablility of plasma membrane and allows influx or eflux of specific ions. limited to the synaptic system
Term
Ligand-Gated ion channel termination
Definition
occurs by diffusion away from receptro
-degradation
-reuptake by presynaptic neuron
Term
Enzyme-Linked Receptor ACtion
Definition
Binding of ligand activates intrinsic enzymatic activity of cytoplasm. limited to endocrine and paracrine systems.
Term
What is the affinity of ligands to enzyme linked receptors
Definition
VERY HIGH
Term
SH2 domain has binding affinity for what?
Definition
Phosphorylated tyrosines
Term
The PTB protein domain has binding affinity for what ?
Definition
Phosphorylated tyrosines
Term
The SH3 Domain has binding affinity for what?
Definition
prolines
Term
The PH domain has binding affinity for what?
Definition
Inositol phospholipids
Term
Receptor Tyrosin Kinase (RTK)
Definition
large transmembrane protein that upon binding of ligand activates kinase activity-->autophosphorylation of tyrosine residues-->binding of signaling proteins-->MAP kinase Cascade
Term
MAP kinase Cascade
Definition
after activation of Enzyme-linked receptor and binding of signaling protein. GTP further activates signaling molecule to activate MAPKKK--ATP-->MAPKK--ATP-->MAPK--ATP-->phosphorylation of membrane protein or phosphorylation of gene regulatory protein
Term
Serine/Threonine Kinase cascade
Definition
Transmembrane enzyme linked protein, 1ligand activates kinase activity-2autophosphorylation
3.SMAD protein binds and is phosphorylated
4.SMAD forms DIMER with another SMAD
5.goes to nucleus and alters gene expression
Term
enzyme-linked receptor termination
Definition
1.receptors cluster
2. vacuole forms, helped by clathrin
3. endosome forms, ligand separates from receptor
4. some receptors are degraded and some are recycled
Term
cytokine receptor
Definition
ligand binding that activates tyrosine kinases. limited to paracrine and autocrine systems
Term
what are the ligands for the cytokine receptor?
Definition
cytokines and some growth factors
Term
cytokine receptor action
Definition
1.separate subunits associated with JAkinases
2. ligand binds forming dimer
3. Bound ligand Activates JAK phospholylation
4.STATS bind
5.JAKS phospohrylate STATS
6.STATs dimerize
7. move to nucleus altering gene expression
Term
Termination of Cytokine Receptors
Definition
-phosophatases
-SOCS
-Endocytic internalization
Term
how do phosphatases terminate cytokine Receptors
Definition
remove tyrosine phosphates from the receptor
Term
how do SOCS proteins inhibit STAT phosphorylation
Definition
by binding and inhbiting JAKS or competing with STATs for phosphotyrosine binding sites
Term
G-protein coupled receptor action
Definition
Binding of ligand activates 3subunit Gprotein which conveys signal to next component in pathway. limited to synaptic, endocrine, paracrine and autocrine systems.
Term
G-protein termination
Definition
-ligands get metabolized or inactivated
-receptor internalization
-receptor phosphorylation desensitizes it
Term
Equilibrium dissociation constant
Definition
Kd=koff/kon=[L][R]/[LR]
Term
Small value for Kd means
Definition
Receptor has high affinity for ligand
Term
Large value for Kd means
Definition
receptor has a low affinity for the ligand
Term
Bmax=
Definition
total number of receptors
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