GMS 6552 Exam 1 with correct answers |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Molecular Drug Targets - correct answer✔✔Receptors-45%
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Enzymes-28%
Hormones-11%
Unknown-7%
Ion Channels-5%
|||\\\
DNA-4%
Channel-Linked (Ionotropic) Receptors - correct answer✔✔Produce cellular effects in |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
milliseconds
Nicotinic ACh receptor |||\\\ |||\\\
GPCRs - correct answer✔✔Effects happen in seconds
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Muscarinic ACh receptor |||\\\ |||\\\
Kinase-linked receptors - correct answer✔✔Effects happen in minutes |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Insulin receptor |||\\\
Receptors linked to gene transcription - correct answer✔✔Effects happen in hours
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Estrogen receptor |||\\\
Heterotrimeric G proteins - correct answer✔✔alpha, beta and gamma subunits |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
GPCR Components - correct answer✔✔More than 800 receptors
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
,7 transmembrane domains
|||\\\ |||\\\
N and C termini
|||\\\ |||\\\ |||\\\
Conformationally flexible |||\\\
Constitutively active |||\\\
GPCR Ligands - correct answer✔✔Hormones, neurotransmitters, chemokine, ions, amino
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
acids, peptides |||\\\
G-proteins - correct answer✔✔a-20 |||\\\ |||\\\ |||\\\ |||\\\
Gas- increases AC |||\\\ |||\\\
Gai - decreases AC
|||\\\ |||\\\ |||\\\
Gaq - increases PLC |||\\\ |||\\\ |||\\\
b(6)y(12)
Why use G proteins - correct answer✔✔Means of amplifying the signal
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
G proteins can regulate more than one effector
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
PKA - correct answer✔✔Phosphorylase Kinase (glycogen breakdown)
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
CREB (gene transcription) |||\\\ |||\\\
L-type Ca channels (heart contraction) |||\\\ |||\\\ |||\\\ |||\\\
Pyruvate Kinase (glycolysis) |||\\\ |||\\\
Hormone Sensitive Lipase (triglyceride breakdown) |||\\\ |||\\\ |||\\\ |||\\\
Kinase-linked receptor signaling - correct answer✔✔No second messenger |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Protein kinase-linked receptors - correct answer✔✔Receptors associated with cytosolic
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
kinases
, Receptor tyrosine kinases |||\\\ |||\\\
Receptor serine/threonine kinases |||\\\ |||\\\
Receptors associated with cytosolic kinases - correct answer✔✔Ligands:
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Prolactin
GH
Interferons
Cytokines
Receptor tyrosine kinases - correct answer✔✔Receptor tyrosine kinases (RTKs) consist of an
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
extracellular ligand |||\\\
binding and dimerization domain, a single hydrophobic
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
transmembrane a-helix and a cytosolic domain with intrinsic |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
tyrosine kinase activity |||\\\ |||\\\
Two types of RTKs - correct answer✔✔Single transmembrane spanning proteins that dimerize
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
when ligand binds (EGF receptor, PGDF receptor)
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Covalently linked dimers (insulin receptor, IGF-1 receptor) |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
PKB/Akt - correct answer✔✔phosphorylate multiple proteins which regulate a wide variety of
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
intracellular events |||\\\
Nuclear Receptor Subfamily - correct answer✔✔Six structural domains:
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
A/B- AF-1 |||\\\
C- DBD
|||\\\
D- Hinge
|||\\\
E- LBD
|||\\\
Molecular Drug Targets - correct answer✔✔Receptors-45%
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Enzymes-28%
Hormones-11%
Unknown-7%
Ion Channels-5%
|||\\\
DNA-4%
Channel-Linked (Ionotropic) Receptors - correct answer✔✔Produce cellular effects in |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
milliseconds
Nicotinic ACh receptor |||\\\ |||\\\
GPCRs - correct answer✔✔Effects happen in seconds
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Muscarinic ACh receptor |||\\\ |||\\\
Kinase-linked receptors - correct answer✔✔Effects happen in minutes |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Insulin receptor |||\\\
Receptors linked to gene transcription - correct answer✔✔Effects happen in hours
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Estrogen receptor |||\\\
Heterotrimeric G proteins - correct answer✔✔alpha, beta and gamma subunits |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
GPCR Components - correct answer✔✔More than 800 receptors
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
,7 transmembrane domains
|||\\\ |||\\\
N and C termini
|||\\\ |||\\\ |||\\\
Conformationally flexible |||\\\
Constitutively active |||\\\
GPCR Ligands - correct answer✔✔Hormones, neurotransmitters, chemokine, ions, amino
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
acids, peptides |||\\\
G-proteins - correct answer✔✔a-20 |||\\\ |||\\\ |||\\\ |||\\\
Gas- increases AC |||\\\ |||\\\
Gai - decreases AC
|||\\\ |||\\\ |||\\\
Gaq - increases PLC |||\\\ |||\\\ |||\\\
b(6)y(12)
Why use G proteins - correct answer✔✔Means of amplifying the signal
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
G proteins can regulate more than one effector
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
PKA - correct answer✔✔Phosphorylase Kinase (glycogen breakdown)
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
CREB (gene transcription) |||\\\ |||\\\
L-type Ca channels (heart contraction) |||\\\ |||\\\ |||\\\ |||\\\
Pyruvate Kinase (glycolysis) |||\\\ |||\\\
Hormone Sensitive Lipase (triglyceride breakdown) |||\\\ |||\\\ |||\\\ |||\\\
Kinase-linked receptor signaling - correct answer✔✔No second messenger |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Protein kinase-linked receptors - correct answer✔✔Receptors associated with cytosolic
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
kinases
, Receptor tyrosine kinases |||\\\ |||\\\
Receptor serine/threonine kinases |||\\\ |||\\\
Receptors associated with cytosolic kinases - correct answer✔✔Ligands:
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Prolactin
GH
Interferons
Cytokines
Receptor tyrosine kinases - correct answer✔✔Receptor tyrosine kinases (RTKs) consist of an
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
extracellular ligand |||\\\
binding and dimerization domain, a single hydrophobic
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
transmembrane a-helix and a cytosolic domain with intrinsic |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
tyrosine kinase activity |||\\\ |||\\\
Two types of RTKs - correct answer✔✔Single transmembrane spanning proteins that dimerize
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
when ligand binds (EGF receptor, PGDF receptor)
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Covalently linked dimers (insulin receptor, IGF-1 receptor) |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
PKB/Akt - correct answer✔✔phosphorylate multiple proteins which regulate a wide variety of
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
intracellular events |||\\\
Nuclear Receptor Subfamily - correct answer✔✔Six structural domains:
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
A/B- AF-1 |||\\\
C- DBD
|||\\\
D- Hinge
|||\\\
E- LBD
|||\\\
