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351 Cards in this Set
- Front
- Back
- 3rd side (hint)
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4 general drug targets |
Ion channels carrier molecules enzymes receptors |
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What are Metabotropic Receptors? |
G-protein coupled membrane protein receptors |
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3 Transcription factor receptors |
Steroid retinoic acid thyroid hormone |
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2 characteristics of Cytokine receptors |
coupled with tyrosine kinase domains activate STATs |
What does ultimately activate? |
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Name 3 miscellaneous drug sites |
Signal pathways structural proteins DNA |
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What do phorbol esters activate in signal pathways? |
PKC |
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PKC is activated by what group of compounds? |
phorbol esters |
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Anti-inflammatory drug for gout: name; target |
Colchicine tubulin
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What is the concept behind law of mass action |
the product of the reactants determines the rate of a reaction |
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What are the variables of a semi-log DR plot? |
%Emax vs log(dose) |
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What is K_D? |
dose that gives E50 |
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What is K_d? |
concentration of free drug that binds half of target molecules |
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What is the value notation for the concentration of drug needed to bind half the concentration of receptor? |
K-d |
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What is a quantal response? |
An effect by a drug that is binary |
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Specificity |
extent of drug action due to effect on a specific target |
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Therapeutic Index and synonym |
Adverse ED50: Therapeutic ED50 Margin of Safety |
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types of Antagonist |
Chemical Pharmacological Physiological/Functional Competitive Noncompetitive Uncompetitive |
6 |
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Chemical antagonist |
reacts with agonist |
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Pharmacological antagonist |
inactivates target; has competitive vs noncompetitive effects on dose-response |
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Physiological/Functional antagonist |
inhibits physiological effect of agonist by stimulating other biological processes that produce an opposing physiological effect |
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What type of antagonist increases ED50/EC50? |
competitive |
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What type of antagonist decreases Emax? |
Noncompetitive |
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What general type of binding molecule has no preference for R or R* state? |
antagonist |
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What do partial agonists prevent? If this can be overcome, how? |
full activation by full agonists this can be overcome by increasing concentration of full agonists |
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Inverse agonists |
bind to constituitively R*; blocks constituitive activity |
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What are constituitively active targets? |
Free targets that are in the R* state; they are free to alternate with R state |
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What isomers have only one chiral center? |
Optical enantiomers |
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3 Structural properties of receptors that can infuence LR binding |
Stereoselectivity Selective blockade by pharmacological antagonists Saturability |
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X-ray crystallography: amplitude of scattered waves indicate what characteristic of an atom |
# of e-s |
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NMR: Irridiation of peak; what is the result? What can be determined from result? What theory is this based on |
causes shift in other peaks approx distances between protons in molecule Nuclear Overhauser Effect |
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What spectroscopic technique is the Nuclear Overhauser Effect associated with? |
NMR |
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2 Limitations of X-ray Crystallography and NMR |
Require mg of sample Not practical for hydrophobic molecules |
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1 Limitation of each: X-ray Crystallography and NMR |
Crystal maybe inconsistent with natural conformation limited to smaller molecules |
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What is the most reliable technique for determining the conformation of a protein? |
structural homology |
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Molecular orbital theory |
used to determine the lowest energy conformations of molecules |
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Isosteres |
pair of molecules that are identical except for a single group of atoms. share similar properties due to similar size, electronegativity or stereochemistry |
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Biosteres |
Compound that is identical to another except for a single group of atoms that results in retention of agonist action |
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Pharmacophore |
Description of 3D features needed for a receptor to bind a ligand |
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Description of 3D features needed for a receptor to bind a ligand |
Pharmacophore |
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Shared pharmacophore for nicotine and Ach |
H-bond acceptor (O vs N) Center of positive charge (protonated N) 4.8 angstrom |
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k1 |
On rate |
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k1[L][R] |
Rate of association |
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k-1[LR] |
rate of dissociation |
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assumptions of the Law of Mass Action |
binding is reversible 2 reactants exist as either bound or free All sites have equal and independent affinity for ligand |
3 |
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4 High Throughput Screening Techniques |
Scintillation proximity assays Amplified Luminescent Proximity Homogenous Assay Surface Plasmon Resonance Fluorescence Resonant Energy Transfer |
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Alpha Screen Assays (3 steps) |
illumination of donor bead produces oxygen radicals diffuse 200nm react with acceptor bead and produce light |
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Alpha Assays |
Amplified Luminescent Proximity Homogenous Assay |
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Surface Plasmon Resonance |
Target proteins bound to gold surface binding of ligand alters refractive index real time measurement |
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Fluorescence Resonant Energy Transfer 3 steps |
illumination of fluorescent chromophore excitation of nearby acceptor chromophore emission of light |
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Scintillation Proximity Assay uses what means? |
radioactive decay |
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What is the fixed variable in displacement plots determined in equlibrium conditions? |
radioligand |
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What value can be determined from semilog plots? |
IC50 |
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IC50 |
the amount of competitor needed to displace 50% of radioligand |
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What are the variables for a Scratchard plot |
bound:free ligand vs bound ligand |
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What is the slope of a Scratchard plot? |
-Kd
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What is the x-intercept of Scratchard plot? |
max concentration of bound ligand |
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Double Reciprocal Plot is also known as... |
Lineweaver-Burk |
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Lineweaver-Burk plot is also known as.... |
double-reciprocal |
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What is the major use for the Double-Reciprocal plot? |
Determine whether an antagonist is competitive or noncompetitive |
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What is the major use for the Hill plot? |
to determine if ligand-receptor binding occurs at independent sites (cooperativity) |
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What value is the x-intercept of the pseudo-hill plot? |
IC50 |
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Ki |
concentration of inhibitor that occupies 50% of receptor/binding affinity of inhibitor |
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Ki vs IC50 |
displace 50% of ligand vs occupy 50% of receptor |
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The Cheng-Prusoff equation is used to calculate what using what? |
Ki with IC50 EC50 [substrate] |
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What interaction-type of inhibitor does the Cheng-Prusoff equation apply to? |
Competitive |
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What causes spare receptors? |
a limitation to a subsequent pathway step |
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in what case is EC50 |
Spare receptors |
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Competitive antagonism |
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Double reciprocal |
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Double reciprocal |
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Hill |
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inverse agonists vs antagonists |
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mulltiple subunit model |
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Noncompetitive antagonism |
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Uncompetitive Antagonism |
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Pseudohill |
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Scratchard |
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Spare receptors with different amounts of inactivator |
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two names for binding |
Allosteric/Heterotropic binding |
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multiple site binding and ligand activation and desensitization |
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desensitization model |
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The extracellular domain of RTKs are rich with what three molecules? |
IgG fibronectin cysteine |
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How does phosphorylation activate a protein? |
Converts nonpolar aminoacid into negatively charged functional group |
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SH2 domain full name |
Src Homology 2 domain |
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function of SH2 |
bind to pY-XXX sequences on RTKs for transphosphorylative activation |
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What on the RTK determines the specificity of action for SH2 domain? |
3 AAs at the C-terminus of pY |
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pY binding domain of RTK commonly activates what protein? |
RasGTPase |
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What kinase does RasGTPase activate? |
MAPK |
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what AA residue of SH2 domain ion-pairs with RTK pY? |
Arginine |
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Grb2 pathway |
SOS RAS RAF MEK MAPK |
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What type of receptor activates Grb2 pathway? |
EGFR |
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PLC pathway and endgame |
PIP2 IP3 DAG Activates PKC |
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What does DAG do? |
binds PKC to membrane |
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What does the PLC pathway ultimately activate? |
PKC |
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What does IP3 do? |
releases Ca2+ from ER activating PKC |
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What type of reaction is performed on PIP2 to produce DAG and IP3? |
Hydrolysis |
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STAT |
Signal transducers and activators of transcription |
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What molecule activates the Jak/STAT pathway when it binds to its receptor? |
cytokine |
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How is STAT phosphorylated directly? |
EGFR |
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JAK |
Janus kinase |
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How is STAT phosphorylated indirectly from membrane receptor activation? |
by JAK |
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5 ways RTK pathway signals are terminated |
Ser/Thr phosphorylation by PKC Heterodimerization w\inactive/truncated receptor Competition with other ligand Dephosphorylation by phosphatases Endocytosis of RTK |
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What are potential outcomes of RTK endocytosis? |
degradation recycling signaling |
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EGFR aka |
ErbB1 Her1 |
2 |
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7 EGFR ligands |
EGF TGF-alpha Heparin B-EGF amphiregulin betacellulin epigen epiregulin |
3 gfs 3 ulin 3 epi |
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Members of EGFR (Her) RTK family |
EGFR ErB2 ErB3 ErB4 |
4 |
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ErbB2 is inactive how? |
no ligand binding site |
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ErbB3 is inactive how? |
little kinase activity |
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ErbB3 ligands |
neuregulin 1 and 2 |
2 |
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ErbB4 ligands x3 +4x |
Heparin B-EGF betacellulin epiregulin neuregulin 1-4
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Hben |
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Insulin RTK family members |
Insulin Receptor Insulin-like GF Receptor Insulin-Related Receptor |
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What are the inactive components of Insulin RTK family? |
dimers of alpha and beta subunits |
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PDGF RTK family members |
PDGF FMS Flt3 c-Kit |
4 |
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FMS contains what receptor? |
Colony stimulating factor 1 receptor |
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Flt3 contains what kinase? |
Fetal Liver Kinase 2 |
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C-kit contains what kind of receptors? |
Mast and stem cell GF receptors |
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What are PDGF ligands derived from? |
GFs that stimulate angiogenesis |
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VEGF coreceptor |
integrin |
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Trk receptors are located in... |
NS |
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Low affinity neurotrophic receptor |
p75 |
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p75 |
neuronal death receptor |
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p75 associated with which RTK family? |
Trk RTK family |
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What is the time frame of RTK signaling? |
hours to days |
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RTK families |
EGFR Insulin PDGFR VEGFR Trk |
5 |
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Notch receptors are for what function? |
cell density |
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how is ligand affinity specified for Notch receptors? |
attached sugars |
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Delta and Jagged membrane proteins are what for what receptor group? |
ligands for notch receptors |
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Gamma-Secretase |
cleaves intracellular domain of notch receptor |
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What protease cleaves the intracellular domain of a notch receptor? |
Gamma-secretase |
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what does the intracellular domain of a notch receptor do when cleaved? |
acts as TF |
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what is the time frame of ligand-gated channels? |
milliseconds |
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Ionotropic receptors |
ligand-gated ion channels |
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what are ligand-gated ion channels commonly involved with? |
synaptic function |
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How do metabotropic receptors activate a signal pathway? |
phosphorylation of G-protein |
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What produces excitatory post-synaptic potentials? |
opening of cation channels |
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what produces inhibitory post-synaptic potential? |
opening of anion channels |
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what NTs activate the opening of ligand-gated cation channels? |
Glutamate Ach Serotonin ATP |
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What NTs activate the opening of ligand-gated anion channels? |
GABA Glycine |
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ligand-gated ion channel family |
Purinergic (ATP) |
ATP |
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ligand-gated ion channel family |
Nicotinic (Ach) |
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ligand-gated ion channel family |
Glutamatergic
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What does the Nernst Equation calculate and with what does it do so? |
Erev external and internal ion concentrations |
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Erev |
reversal potential |
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reversal potential |
voltage at which there is no net current through a single ion-selective channel |
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What produces the resting membrane potential? |
open K+ channels |
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What two components are highest in concentration within the cell during resting potential? |
K+ impermeant anions |
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What two components are highest in concentration outside the cell during resting potential? |
Na+ Cl- |
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What is the direction of the overall concentration gradient across the cell membrane? |
intracellular to extracellular |
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What force drives K+ during resting potential, and where does it force it? |
Concentration gradient outside |
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What is the process of producing an excitatory post-synaptic potential? |
depolarization |
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What is the process of producing an inhibitory post-synaptic potential? |
hyperpolarization |
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Hyperpolarization happens when.... |
anion channels open to allowing them to enter cell |
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depolarization happens when |
cation channels open allowing them to exit the cell |
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What 2 types of receptors induce hyperpolarization? |
GABA Glycine |
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GABA |
gamma-aminobutyric acid |
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GABA_C is found where? |
in the retina |
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2 facts about GABA_C |
contains rho subunits insensitive to modulators |
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Benzodiazepines and barbiturates are what to which receptor? |
noncompetitive coagonists or allosteric modulators GABA_a |
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Which coagonist of GABA_A can act as a full agonist? |
Barbiturates |
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What BZ site does Benzodiazepine have the highest affinity? |
BZ1 |
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What are two antagonists of GABA_A? |
bicuculline picrotoxin |
q |
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bicuculline and picrotoxin are antagonists of which receptor? |
GABA_A |
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3 agonists of Glycine ligand-gated anion channels |
glycine taurine beta-alanine |
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antagonist of glycine ligand-gated anion channels |
strychnine |
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what type of antagonist is strychnine for glycine ligand gated anion channels? |
allosteric inhibitor |
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What ions pass through Glycine-gated ion channels? |
Cl- |
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Depolarization involves which two ion species? |
Na+ Ca2+ |
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3 major Depolarizing Ligand-gated ion channel families |
Nicotinic Serotonin Glutamate |
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What molecule is the major excitatory NT? |
Glutamate |
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Serotonin ligand-gated ion channel is also known as: |
5HT_3 |
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What depolarizing ligand-gated ion channel family requires a threshold potential to be reached before generating an action potential? |
Nicotinic |
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What does a motor neuron's post-synaptic action potential induce? |
release of calcium ions from sarcoplasmic reticulum in muscle cells |
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Nicotinic receptors are located where? |
neuro-muscular junctions |
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Antagonist of Nicotinic receptors |
curare |
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Depending on subunit structure, what do nicotinic ligand-gated ion channels allow to pass? |
Na+ K+ Ca2+ |
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What is the homolog to Nicotinic receptors? |
Serotonin/5HT_3 receptors |
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How many subunits make up the channel in serotonin receptors? |
5 |
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What is the large-scale function for Serotonin receptors? |
fight-or-flight response |
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What ligand-gated ion channel family is located in the amygdala? |
Serotonin/5HT_3 |
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What do Serotonin/5HT_3 receptors regulate? |
release of dopamine, Ach, GABA |
3 |
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What is a major antagonist of Serotonin/5HT_3 receptors? |
Ondansetron |
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This ligand-gated ion channel can be activated metabotropically: |
Glutamatergic |
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Glutamate ligand-gated ion channel clusters are maintained by what and where? |
scaffold protein PSD-95 Post synapse |
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What do glutamate receptors do besides depolarize? |
activate signaling molecules |
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Members of Glutamate receptor family |
NMDA AMPA |
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NMDA has how many subunits? |
4
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What do NR1 subunits bind for which receptor? |
coagonist glycine or serine NMDA |
AA |
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What do NR2 subunits bind for which receptor? |
agonist glutamate or aspartate NMDA |
2 Basic forms of AAs |
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Which NMDA subunits bind coagonists? |
NR1 |
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which NMDA subunits bind agonists? |
NR2 |
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modulators of NMDA receptors |
Zn Polyamines Aminoglycosides Redox |
4 |
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What is Zinc in terms of NMDA modulation? |
voltage-independent competitive inhibitor |
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What do polyamines do in terms of NMDA modulation? |
potentiate glutamate action |
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What are aminoglycosides? |
antibiotics w\neurotoxin action |
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NMDA receptors |
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NMDA receptor |
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Antagonist to NMDA receptors: |
PCP |
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PCP is an antagonist to which receptors (2)? What kind of antagonist is it? |
NMDA Nicotinic noncompetitive |
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Which ligand-gated ion channel is voltage-dependent for activation? how is this done? |
NMDA Forcing out of Mg2+ from channels |
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What ligand-gated ion channel activates another voltage-activated ligand-gated channel? |
AMPA |
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Agonist for AMPA receptors |
glutamate |
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where in the synapse is glutamate release from? |
presynaptic membrane |
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What are the AMPA subunits? |
GluR1-4 |
Agonist |
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What does GluR2 subunit do? |
prevents permeation by Ca2+ |
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Which ligand-gated ion channel requires more than one agonist binding for activation? |
AMPA |
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AMPA receptor antagonists: |
kynurenic acid (endogenous) CNQX (also for kainate receptors) |
K c |
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What are the secondary messenger systems activated by the NMDA induced cation influx? |
Calmodulin CaMKII |
Ca2+ |
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CaMKII serves what purposes? |
sensitizes AMPA Recruits AMPA to post-synaptic membrane |
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How is NMDA signal amplified? |
NMDA Ca2+ CaMKII AMPA sensitization/recruitment |
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Kynurenic acid is derived from? What receptor is it antagonistic towards? |
tryptophan AMPA |
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What is a tryptophan metabolite that acts as an AMPA antagonist? |
Kynurenic Acid |
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Describe the 3 main structural components of GPCR? |
7 transmembrane alpha-helices 3 intracellular loops Extracellular domain |
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what may the extracellular domain of a GPCR be regulated by? |
glycosylation |
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The intracellular loops provide what for what two targets? |
binding sites G-Protein arrestin |
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What does the G-protein bind with during GPCR resting state? |
third intracellular loop C' terminal Strand |
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How many intracellular binding loops are there in GPCR? |
3 |
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How many transmembrane subunits are there in a GPCR? what is there secondary structure? |
7 alpha helices |
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GPCR: how can the 3-d conformation of intracellular loops be maintained? |
S-S |
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GPCR: role of glycosylation |
regulate extracellular domain
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GPCR: role of S-S |
maintain intracellular loop 3-D conformation |
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What are the components of the G-protein? |
Alpha beta gamma |
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How are G proteins activated? |
GDP-GTP exchange |
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What happens upon G-protein dissociation? |
beta and gamma dimer dissociates from alpha |
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Golf(alpha) |
olfaction |
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Gt(alpha) |
vision |
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Gi(alpha) |
activates ion channels inhibits cAMP, adenylylcyclase, phospholipase |
activates 1 inhibits 3 |
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Gq(alpha) |
stimulates PLC increases DAG, IP3 |
stimulates 1 increases 2 |
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Gs(alpha) |
Stimulates adenylylcyclase Increase cAMP |
Stimulates 1 Increase 1 |
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What is adenylylcyclase activated by? |
Galpha subunits of certain G-proteins |
subunits |
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Forskolin |
activates adenylate cyclase increases cAMP |
activates increases |
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Cholera toxin |
ADP-ribosylation of G(alpha)s subunits and Gi |
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PGCR |
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adenylylcyclase GPCR complex |
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GPCR |
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neuregulin 1 and 2 are the only ligands to which EGFR RTK? |
ErbB3 |
3 |
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Heparin B-EGF is a ligand to which EGFR RTK? |
ErbB4 |
4 |
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betacellulin is a ligand to which EGFR RTK? |
ErbB4 |
4 |
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epiregulin is a ligand to which EGFR RTK? |
ErbB4 |
4 |
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neuregulin 1-4 are ligands to which EGFR RTK? |
ErbB4 |
4 |
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SOS>RAS>RAF>MEK>MAPK |
Grb2 pathway |
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Jak phosphorylates what? |
STAT |
indirect |
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ErbBn receptor is a member of which receptor family? |
EGFR RTK family |
RTK family |
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EGFR, Insulin, PDGFR, VEGEFR, Trk receptor families are of what receptor variant? |
RTK |
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integrin is a what to what RTK family? |
coreceptor VEGFR RTK family |
co |
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FMS, Flt3, and c-kit are members of which RTK family? |
PDGF RTK family |
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Her RTK family aka: |
EGFR RTK family |
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MAPK is phosphorylated by which protein? |
RasGTPase
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phosphatase |
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What are the ligands for notch receptors? |
jagged delta |
2 |
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Strychnine |
inhibitor of glycine-gated chloride channel |
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GluR1-4 are subunits for which ligand-gated ion channel? |
AMPA |
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These ligand-gated ion channels regulate dopamine, Ach, and GABA release: |
Serotonin |
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Ondansetron is what for what? |
inhibitor
Serotonin-gated cation channels |
cation channel |
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What ligand-gated ion channel is made of 4 subunits? |
NMDA |
cation |
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Curare is what for what? |
antagonist
Nicotinic receptors |
cation channel |
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In addition to depolarization, these ligand-gated cation channels also activate signaling molecules: |
Glutamatergic receptors |
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Which ligand-gated ion channel form postsynaptic membrane clusters? |
Glutamatergic receptors |
cation |
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Ligands of glucocorticoid receptors: |
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2 |
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Ligands for thyroid receptors: |
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4 |
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Wnt Receptor pathway |
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Type II nuclear receptors |
type |
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Type I nuclear receptors |
type |
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Wnt pathway |
GPCR pathway |
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Hedge hog pathway |
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GABAb pathway: GABAb is an example of what other than a ligand-gated anion channel? |
metabotropic |
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ligand binding domain is described as what for what type of receptor? |
venusfly trap metabotropic |
g-protein coupled |
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BARK is associated with which pathway? |
beta-adrenergic pathway |
GPCR pathway |
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Noble prize winners and accomplisment |
Rob Lefkowitz and Brian Kobilka Radioligand binding assays to show existence of GPCR |
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PKA: full name and action |
cAMP dependent protein kinase phosphorylation of GPCR intracellular domains |
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What is GPCR desensitization performed by? |
phosphorylation of intracellular domains by PKA and GRK |
2 kinases |
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GRK |
GPCR Kinase |
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What are the potential outcomes of GPCR densensitizing phosphorylation? |
Endocytosis/translocation Arrestin binding GTP hydrolysis Oligomerization |
4 |
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What does arrestin binding accomplish for the regulation of which receptor family? |
prevents G-protein binding GPCR |
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Which desensitization endpoints lead to alternate pathways in GCPRs? |
Oligomerization Arrestin binding |
2 |
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Which desensitization endpoints lead to alternate pathways in GPCRs? |
Oligomerization Arrestin binding |
2 |
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What are two ion channel variants of rhodopsin GPCR? |
channelrhodopsin Halorhodopsin |
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betaAdrenergic receptors are part of which family? |
GPCR |
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BARK is what kind of kinase? |
GRK |
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cAMP removes regulatory subunits from this kinase which in turn phosphorylates which type of kinase? |
PKA GRK |
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2 Beta-blockers |
atenolol propanolol |
olol |
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What activates adenylyl cyclase? |
Galpha subunits |
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what does adenylyl cyclase produce? |
cAMP |
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what produces cAMP and what does it in turn activate? |
adenylyl cyclase PKA |
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what nonkinase target does PKA phosphorylate? |
CREB |
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Which receptor family are biased and balanced agonism variants involved with? How are these variants made possible? |
GPCR
Plasticity of 7TMRS |
7
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Where is GPCR phosphorylated by GRK and what does this accomplish? |
C'terminus converts GPCR conformation to have bias for beta-arrestin pathways |
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What type of molecule acts as the agonist to SHH? what does this complex do? |
cholesterol inhibits PTCH |
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What is a smooth receptor? |
GPCR involved with SSH |
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What allows SSH-cholesterol to be secreted? |
Dsp |
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What does PTCH inhibit? |
smooth GPCR |
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smooth GPCR is inhibited by what? |
PTCH |
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What type of GPCR does the Wnt pathway involve? |
Frizzled |
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What pathway is frizzled GPCR involved in? |
Wnt pathway |
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What does Wnt pathway prevent? |
beta Catenin degradation |
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beta catenin is involved in which pathway? |
Wnt |
GPCR |
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what kind of molecule acts as secretin GPCR agonists from where? |
polypeptide hormones from intestine, pancreas |
2 locations
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polypeptide hormones from the intestine and pancreas are agonists for which GPCRs? |
Secretin receptors |
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large extracellular N-terminal regions are a unique feature to this GPCR: |
Adhesion GPCR |
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Unique feature of Adhesion GPCRS |
large extracellular N-terminal regions |
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what molecules can associate with functional domains of adhesion GPCRs? |
TKs integrins cadherins |
3 |
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TKs, integrins, and cadherins can associate with the functional domain of these GPCRs: |
Adhesion GPCRs |
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Estrogen Receptors are an example of what? |
Type I nuclear receptor |
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What nuclear receptor family complexes w\HS proteins when inactive? |
Type I |
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What does ligand binding of Type I receptors cause? |
dissociation of HS proteins and dimerization |
2 steps of activation |
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What does an active Type I receptor do? |
binds to nuclear receptors which initiate transcription of HRE |
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What is the ultimate subcellular endpoint of Type I receptor activation? |
Transcription of HRE |
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Transcription of HRE is the ultimate subcellular endpoint of which receptor family? |
Type I |
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Tamoxifen |
Estrogen Receptor-targeting drug |
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tamoxifen acts as an antagonist in which tissue variant? |
mammory |
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tamoxifen acts as what in bone tissue? |
agonist
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tamoxifen acts as what in mammory tissue? |
antagonist |
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tamoxifen acts as what in uterine endothelial tissue? |
agonist |
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Thyroid receptors are an example of which receptor family? |
Type II |
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RXR |
retinoid x receptor |
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Inactive type II receptors dimerize with what? what does this dimer complex with? |
RXR corepressor proteins |
specific type II receptor |
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What does inactive RXR bind to? |
DNA |
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What receptor family does RXR belong to? |
Type II |
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Thyroid receptor ligands are collectively known as: |
thyroamines |
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What does activated thyroid receptor increase and regulate? |
basal metabolic rate heart rate cell differentiation |
2 and one |
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What processes do thyroid hormones regulate? |
hibernation body temperature neuronal activity |
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What receptor family is targeted by T3? what does this regulate? |
Type II body temp metabolism |
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What is necessary for thyroid hormone to bind it's respective receptor? |
Heterodimerized w\RXR |
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Heterodimerization w\RxR allows what for what receptor family? |
ligand binding of Type II receptor |
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When binding to DNA, which nuclear receptor family(ies) form homodimers? Heterodimers? |
Type I and III Type II |
2 and 1 |
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Retinoic Acid Receptor agonist |
Vitamin A |
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Vitamin A is the agonist to which receptor? |
Retinoic Acid Receptor |
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What receptor family does Retinoic Acid Receptor belong to? |
Type III |
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what does Vitamin A induce? |
cell differentiation |
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What does Vitamin D receptor regulate? |
intestinal absorption of Ca2+ and phosphate |
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Vitamin D prohormones |
ergocalciferol cholecalciferol |
calciferol |
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Aldosterone receptor aka and functions: |
Mineralocorticoids K+ excretion Na+ reabsorption expression of ion pumps |
3 functions |
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Dopamine Precursor |
Tyrosine |
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Tyrosine is the precursor to which NT? |
dopamine |
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Striatal Dopamine deficiency is associated with |
Parkinson's |
disease |
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Parkinson's disease is associated with deficiency of this compound in this location |
Dopamine Striatum |
NT |
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Classic symptoms of PD |
resting tremor rigidity bradykinesia |
triad |
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PD Neuropathology |
Extrapyramidal Dopaminergic Nigrostriatal |
3 Pathway |
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Components of the Striatum |
Basal Ganglia Substantia Nigra |
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Components of the A10 neural pathway |
Frontal cortex Nuclear Accumbens Ventral Tegmentum |
3 |
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Components of the A9 Neural pathway |
Basal ganglia substantia nigra |
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Extrapyramidal dopaminergic nigrostriatal system |
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Endogenous neurotoxicants |
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haloperidol |
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lipid peroxidation |
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MAO oxidation of catecholamine NTs |
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MAO oxidation of catecholamine NTs |
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MPTP formation |
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MPTP to MPP+ |
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Normal vs Parkinson's |
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Paraquat |
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Pyridines and MPP+ neurodegeneration |
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Reduction of quinone |
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