GMS 6552 Exam with !| !| !| !|
accurate detailed !| !|
solutions
What is the most common molecular drug target?
!| !| !| !| !| !| !| !|
Enzymes
Hormones & Factors !| !|
Receptors
Ion Channels
!|
DNA - Correct answer ✔Receptors
!| !| !| !|
Channel-linked (ionotropic) receptor time scale - Correct answer
!| !| !| !| !| !| !| !|
✔Milliseconds
G-protein coupled receptor time scale - Correct answer ✔Seconds
!| !| !| !| !| !| !| !|
Kinase-linked receptor time scale - Correct answer ✔Minutes
!| !| !| !| !| !| !|
Nuclear receptor time scale - Correct answer ✔Hours
!| !| !| !| !| !| !|
,Number of GPCR receptors - Correct answer ✔>800
!| !| !| !| !| !| !|
GPCR Ligands - Correct answer ✔Hormones, neurotransmitters,
!| !| !| !| !| !| !|
chemokine, ions, amino acids, peptides !| !| !| !|
G alpha proteins - Correct answer ✔20
!| !| !| !| !| !|
G beta proteins - Correct answer ✔6
!| !| !| !| !| !|
G gamma proteins - Correct answer ✔12
!| !| !| !| !| !|
Why use G proteins? - Correct answer ✔Amplify signal, regulate more
!| !| !| !| !| !| !| !| !| !| !|
than one effector
!| !|
signal transduction cascade of cyclic AMP - Correct answer ✔Adrenaline
!| !| !| !| !| !| !| !| !| !|
binds to adrenergic receptor --> alpha GTP activates adenylyl cyclase -->
!| !| !| !| !| !| !| !| !| !| !|
ATP converted to cAMP --> PKA is activated --> transcription changes
!| !| !| !| !| !| !| !| !| !|
What proteins does PKA phosphorylate - Correct answer
!| !| !| !| !| !| !| !|
✔phosphorylase kinase, L-type Ca channels, pyruvate kinase, CREB, !| !| !| !| !| !| !| !|
hormone sensitive lipase !| !|
Phospholipase C activation activates - Correct answer ✔DAG, IP3
!| !| !| !| !| !| !| !|
, Kinase linked receptor signaling - Correct answer ✔hormone binds -->
!| !| !| !| !| !| !| !| !| !|
change in kinase and/or phosphatase activity
!| !| !| !| !|
Protein kinase linked receptors - Correct answer ✔cytosolic kinases,
!| !| !| !| !| !| !| !| !|
tyrosine kinases, serine/threonine kinases
!| !| !|
Cytosolic kinases - Correct answer ✔Ligand binds --> receptors dimerize
!| !| !| !| !| !| !| !| !| !|
--> JAK activated --> STAT activated --> dimerization and nuclear
!| !| !| !| !| !| !| !| !| !|
translocation
Receptor tyrosine kinases - Correct answer ✔an extracellular ligand
!| !| !| !| !| !| !| !| !|
binding and dimerization domain, a single hydrophobic transmembrane
!| !| !| !| !| !| !| !|
alpha helix and a cytosolic domain with intrinsic tyrosine kinase activity
!| !| !| !| !| !| !| !| !| !|
Types of receptor tyrosine kinases - Correct answer ✔single
!| !| !| !| !| !| !| !| !|
transmembrane spanning proteins that dimerize when ligand binds or !| !| !| !| !| !| !| !| !|
covalently linked dimers !| !|
PKB/Akt proteins effects - Correct answer ✔Glycogen synthesis, protein
!| !| !| !| !| !| !| !| !|
synthesis, glycolysis, glucose transport, transcription of specific gene
!| !| !| !| !| !| !|
Serine/threonine receptor kinases - Correct answer ✔ligand binds to !| !| !| !| !| !| !| !| !|
type 2 receptor, type 2 receptor dimerizes type 1 receptor, type 1
!| !| !| !| !| !| !| !| !| !| !| !|
receptor activates SMAD 2, Smad 2 binds to smad 4
!| !| !| !| !| !| !| !| !|
accurate detailed !| !|
solutions
What is the most common molecular drug target?
!| !| !| !| !| !| !| !|
Enzymes
Hormones & Factors !| !|
Receptors
Ion Channels
!|
DNA - Correct answer ✔Receptors
!| !| !| !|
Channel-linked (ionotropic) receptor time scale - Correct answer
!| !| !| !| !| !| !| !|
✔Milliseconds
G-protein coupled receptor time scale - Correct answer ✔Seconds
!| !| !| !| !| !| !| !|
Kinase-linked receptor time scale - Correct answer ✔Minutes
!| !| !| !| !| !| !|
Nuclear receptor time scale - Correct answer ✔Hours
!| !| !| !| !| !| !|
,Number of GPCR receptors - Correct answer ✔>800
!| !| !| !| !| !| !|
GPCR Ligands - Correct answer ✔Hormones, neurotransmitters,
!| !| !| !| !| !| !|
chemokine, ions, amino acids, peptides !| !| !| !|
G alpha proteins - Correct answer ✔20
!| !| !| !| !| !|
G beta proteins - Correct answer ✔6
!| !| !| !| !| !|
G gamma proteins - Correct answer ✔12
!| !| !| !| !| !|
Why use G proteins? - Correct answer ✔Amplify signal, regulate more
!| !| !| !| !| !| !| !| !| !| !|
than one effector
!| !|
signal transduction cascade of cyclic AMP - Correct answer ✔Adrenaline
!| !| !| !| !| !| !| !| !| !|
binds to adrenergic receptor --> alpha GTP activates adenylyl cyclase -->
!| !| !| !| !| !| !| !| !| !| !|
ATP converted to cAMP --> PKA is activated --> transcription changes
!| !| !| !| !| !| !| !| !| !|
What proteins does PKA phosphorylate - Correct answer
!| !| !| !| !| !| !| !|
✔phosphorylase kinase, L-type Ca channels, pyruvate kinase, CREB, !| !| !| !| !| !| !| !|
hormone sensitive lipase !| !|
Phospholipase C activation activates - Correct answer ✔DAG, IP3
!| !| !| !| !| !| !| !|
, Kinase linked receptor signaling - Correct answer ✔hormone binds -->
!| !| !| !| !| !| !| !| !| !|
change in kinase and/or phosphatase activity
!| !| !| !| !|
Protein kinase linked receptors - Correct answer ✔cytosolic kinases,
!| !| !| !| !| !| !| !| !|
tyrosine kinases, serine/threonine kinases
!| !| !|
Cytosolic kinases - Correct answer ✔Ligand binds --> receptors dimerize
!| !| !| !| !| !| !| !| !| !|
--> JAK activated --> STAT activated --> dimerization and nuclear
!| !| !| !| !| !| !| !| !| !|
translocation
Receptor tyrosine kinases - Correct answer ✔an extracellular ligand
!| !| !| !| !| !| !| !| !|
binding and dimerization domain, a single hydrophobic transmembrane
!| !| !| !| !| !| !| !|
alpha helix and a cytosolic domain with intrinsic tyrosine kinase activity
!| !| !| !| !| !| !| !| !| !|
Types of receptor tyrosine kinases - Correct answer ✔single
!| !| !| !| !| !| !| !| !|
transmembrane spanning proteins that dimerize when ligand binds or !| !| !| !| !| !| !| !| !|
covalently linked dimers !| !|
PKB/Akt proteins effects - Correct answer ✔Glycogen synthesis, protein
!| !| !| !| !| !| !| !| !|
synthesis, glycolysis, glucose transport, transcription of specific gene
!| !| !| !| !| !| !|
Serine/threonine receptor kinases - Correct answer ✔ligand binds to !| !| !| !| !| !| !| !| !|
type 2 receptor, type 2 receptor dimerizes type 1 receptor, type 1
!| !| !| !| !| !| !| !| !| !| !| !|
receptor activates SMAD 2, Smad 2 binds to smad 4
!| !| !| !| !| !| !| !| !|