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
What activates Kinase-Linked Receptors
Protein Mediators
Cytokines, Growth Factors, Hormones
What process do Kinase-Linked Receptors control
Cell Division, Metabolism, Growth, Inflammation
Main Types of Kinase-Linked Receptors
Receptor Tyrosine Kinases
Receptor Serine/Threonine Kinase
Cytokine Receptors
What are Receptor Tyrosine Kinases
Phosphorylation of Tyrosine and then is incorporated intracellular
Regulate gene transcription
What binds to RTKs
Growth Factors
What are Receptor Serine/Threonine Kinases
Phosphorylates serine/threonine residues
What are Cytokine Receptors
Receptors that when binded to activate kinases in the intracellular domain
Regulates Gene Transcription
What are the characteristics of Ion Channels
Selectivity: What the channel is permeable to
Gating: What opens the channel
Ionotropic Receptors
Ligand-Gated Ion Channel
Metabotropic Receptors
G-Protein Coupled Receptors
What are the 4 types of Ion Channels
Cys-loop type
Ionotropic Glutamate
P2X Type
Ca2+ Type
Main families of transporters
ATP Binding Cassette (ABC)
Solute Carrier (SLC)
P-Type ATPase
ATP Binding Cassette (ABC)
Use ATP hydrolysis to fuel efflux transporters
Solute Carrier (SLC)
Involved in influx of small molecules
P-Type ATPase
Na+/K+ ATPase
Helps maintain membrane potential
