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Exam (elaborations)

GMS 6552 Exam 1

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Agonist Activation of GPCR - answer-Ligand binds Promotes conformational changes Increase in R Inverse Agonist Inhibition of GPCR - answer-Ligand binds Stabilizes inactive receptor conformations Antagonist Inhibition of GPCR - answer-Do not effect basal constitutive signaling Do not affec...

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  • September 29, 2024
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  • 2024/2025
  • Exam (elaborations)
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  • GMS 6552
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TOPDOCTOR
GMS 6552 EXAM 1 2025
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

RXR partnered ligands - answer-9-Cis RA + X

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