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Molecular Drug Targets - Answer Receptors-45%
Enzymes-28%
Hormones-11%
Unknown-7%
Ion Channels-5%
DNA-4%
,Channel-Linked (Ionotropic) Receptors - Answer Produce cellular
effects in milliseconds
Nicotinic ACh receptor
GPCRs - Answer Effects happen in seconds
Muscarinic ACh receptor
Kinase-linked receptors - Answer Effects happen in minutes
Insulin receptor
Receptors linked to gene transcription - Answer Effects happen in
hours
Estrogen receptor
Heterotrimeric G proteins - Answer alpha, beta and gamma subunits
GPCR Components - Answer More than 800 receptors
7 transmembrane domains
N and C termini
Conformationally flexible
Constitutively active
GPCR Ligands - Answer Hormones, neurotransmitters, chemokine,
ions, amino acids, peptides
, G-proteins - Answer a-20
Gas- increases AC
Gai - decreases AC
Gaq - increases PLC
b(6)y(12)
Why use G proteins - Answer Means of amplifying the signal
G proteins can regulate more than one effector
PKA - 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 - Answer No second messenger
Protein kinase-linked receptors - Answer Receptors associated with
cytosolic kinases
Receptor tyrosine kinases
Receptor serine/threonine kinases
Receptors associated with cytosolic kinases - Answer Ligands:
Prolactin
GH