Lecture 1 - Drug Action Flashcards
What are the four types of proteins drugs act on?
Receptors
Ion Transporters
Enzymes
Transporters
What are the three main families of Receptors
G-Protein
Kinase-Linked
Nuclear Receptors
What class of receptor are GPCRs?
Metabotropic Receptors
GPCR N-Terminus
Extracellular
Site of Agonist Binding
GPCR C-Terminus
Intracellular
G-Protein coupled to an effector
How fast are GPCRs
Slow acting
GPCRs Class A
Neurotransmitters
Rhodosin Family
GPCRs Class B
Peptide Hormones
Secretin/Glucagon
GPCRs Class C
Metabotropic Glutamate and Ca2+
G-Protein: Ga(s)
Stimulates Adenylate Cyclase –> Increase cAMP
G-Protein: Ga(i)
Inhibits Adenylate Cyclase –> Decrease cAMP
G-Protein: Ga(q)
Activates Phospholipase C –> Increase IP3 and DAG
G-Protein: Ga(o)
beta and gamma subunits dissociate and cause effects
G-Protein: Ga(12/13)
Activates Rho & Rho Kinase
(Cell Growth)
G(beta/gamma)
Membrane Hyperpolarization
Activates K+ Channels
Inhibits voltage-gated Ca2+
Activate GPCR Kinase