GMS 6552 Exam 1 Questions and Answers 100% Accurate!!
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
Interferons
Cytokines
Receptor tyrosine kinases - 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 - ANSWER-Single transmembrane spanning proteins that dimerize when ligand binds (EGF receptor, PGDF receptor)
Covalently linked dimers (insulin receptor, IGF-1 receptor)
PKB/Akt - ANSWER-phosphorylate multiple proteins which regulate a wide variety of intracellular events
Nuclear Receptor Subfamily - ANSWER-Six structural domains:
A/B- AF-1
C- DBD
D- Hinge
E- LBD
F- AF-2
Steroid class receptors - ANSWER-GR, MR, PR, AR, ER
RXR partnered receptors - ANSWER-TR, RAR, VDR, PPAR, a, b, y
Orphan receptors - ANSWER-COUP-TF, HNF-4
Steroid receptor ligands - ANSWER-Steroids
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