GMS 6552 FINAL EXAM ACTUAL QUESTIONS AND
ANSWERS SURE A+
✔✔Enhancement of tumor progression - ✔✔-Refractory to growth inhibition
-Increased TGF-ß production
-Decreased immunesurveillance
-Increased ECM production
-Angiogenesis
-Decreased cell-cell adhesion
-Increased motility
-Transdifferentiation (EMT)
-Increased COX-2 expression
✔✔TGFB pathway - ✔✔-TGFB ligand
-Dimerization of receptors and activation of serine/threonine kinase activity
-Receptor phosphorylation of downstream substrates
-Smad oligomerization and nuclear translocation
-Regulation of gene transcription
-Cell cycle arrest or altered cell morphology, EMT
✔✔G-protein coupled receptors - ✔✔Responsive to a wide variety of physiological
stimuli
Most-widely used drug targets
✔✔GPCR Examples - ✔✔Muscarininc AchRs
Histamine
Serotonin
Dopamine
Opioid
Rhodopsin
✔✔GPCR Families - ✔✔Rhodopsin (A)
Secretin (B)
Metabotropic glutamate (C)
Adhesion of GPCRs
Fungal pheromone
cAMP receptors
Frizzled/Smoothened
✔✔Family A GPCR - ✔✔Largest
Small N-terminus
Cysteines for disulfide bonds
Proline residues
Palmitoylaiton site in C-tail
Conserved DRY motif in IC2 loop
, ✔✔Family A Examples - ✔✔Biogenic amines
CCK
Bradykinin
FSH
Melatonin
✔✔Family B GPCR - ✔✔30 receptors for a variety of peptide hormones
Long N-terminus
Cysteines
No palmitoylation site
No DRY motif
✔✔Family B Examples - ✔✔Calcitonin
PTH
Glucagon
Latrotoxin
✔✔Family C GPCR - ✔✔Very long N-terminus
Cysteines
No palmitoylation site
Very short 3rd IC loop
✔✔Family C Examples - ✔✔Metabotropic glutamate
Metabotropic GABA
Calcium
Vomeronasal pheromone
Taste
✔✔Agonist Activation of GPCR - ✔✔Ligand binds
Promotes conformational changes
Increase in R
✔✔Inverse Agonist Inhibition of GPCR - ✔✔Ligand binds
Stabilizes inactive receptor conformations
✔✔Antagonist Inhibition of GPCR - ✔✔Do not effect basal constitutive signaling
Do not affect receptor conformation when they bind
✔✔GPCR Full Agonist - ✔✔Produces full biological response
✔✔GPCR Partial Agonist - ✔✔Can only produce partial biological response even at
saturating concentrations
✔✔GPCR Inverse Agonist - ✔✔Suppresses basal activity
ANSWERS SURE A+
✔✔Enhancement of tumor progression - ✔✔-Refractory to growth inhibition
-Increased TGF-ß production
-Decreased immunesurveillance
-Increased ECM production
-Angiogenesis
-Decreased cell-cell adhesion
-Increased motility
-Transdifferentiation (EMT)
-Increased COX-2 expression
✔✔TGFB pathway - ✔✔-TGFB ligand
-Dimerization of receptors and activation of serine/threonine kinase activity
-Receptor phosphorylation of downstream substrates
-Smad oligomerization and nuclear translocation
-Regulation of gene transcription
-Cell cycle arrest or altered cell morphology, EMT
✔✔G-protein coupled receptors - ✔✔Responsive to a wide variety of physiological
stimuli
Most-widely used drug targets
✔✔GPCR Examples - ✔✔Muscarininc AchRs
Histamine
Serotonin
Dopamine
Opioid
Rhodopsin
✔✔GPCR Families - ✔✔Rhodopsin (A)
Secretin (B)
Metabotropic glutamate (C)
Adhesion of GPCRs
Fungal pheromone
cAMP receptors
Frizzled/Smoothened
✔✔Family A GPCR - ✔✔Largest
Small N-terminus
Cysteines for disulfide bonds
Proline residues
Palmitoylaiton site in C-tail
Conserved DRY motif in IC2 loop
, ✔✔Family A Examples - ✔✔Biogenic amines
CCK
Bradykinin
FSH
Melatonin
✔✔Family B GPCR - ✔✔30 receptors for a variety of peptide hormones
Long N-terminus
Cysteines
No palmitoylation site
No DRY motif
✔✔Family B Examples - ✔✔Calcitonin
PTH
Glucagon
Latrotoxin
✔✔Family C GPCR - ✔✔Very long N-terminus
Cysteines
No palmitoylation site
Very short 3rd IC loop
✔✔Family C Examples - ✔✔Metabotropic glutamate
Metabotropic GABA
Calcium
Vomeronasal pheromone
Taste
✔✔Agonist Activation of GPCR - ✔✔Ligand binds
Promotes conformational changes
Increase in R
✔✔Inverse Agonist Inhibition of GPCR - ✔✔Ligand binds
Stabilizes inactive receptor conformations
✔✔Antagonist Inhibition of GPCR - ✔✔Do not effect basal constitutive signaling
Do not affect receptor conformation when they bind
✔✔GPCR Full Agonist - ✔✔Produces full biological response
✔✔GPCR Partial Agonist - ✔✔Can only produce partial biological response even at
saturating concentrations
✔✔GPCR Inverse Agonist - ✔✔Suppresses basal activity
