Drug Targets Flashcards
Describe the GPCR Cycle.
The classification of G-Protein Families is based on ___________ .
G alpha subunit - Induced Effects
Describe how to turn off the signal transduction pathway started by the GPCR.
GRK (GPCR Kinase), Beta-Arrestin, Protein Phosphatase
List the different Protein Domains that are present within the Receptor Tyrosine Kinases.
- Ligand-Binding Domain
- Transmembrane Domain
- Tyrosine Kinase Domain
What is the purpose of Adaptor Proteins?
Adaptor Proteins provide means to create a sequential transduction pathway.
GEFs (SOS) are going to activate Monomeric GTPases
List, in order, the growth factor pathways in cancer.
Growth Factor –> RTK –> G-Protein –> RAF –> MEK –> ERK –> Transcription Factor
Describe the function of targeted anticancer drugs.
Inhibits upregulated growth factor (GF) signaling
Ligand-Activated transcription factors that modulate gene expression are an example of ________ .
Nuclear Receptors
True or False.
The effects of a nuclear receptor cannot persist after the agonist concentration has been reduced to zero.
FALSE
You will still have effects occuring because it takes a long time for the TFs to activate RNA Polymerase II and cause an effect!
What are the various functions of:
- Gs
- Gi
- Gq
- Gs: Adenylate Cyclase Activation (Can activate SRC Tyrosine Kinase)
- Gi: Adenylate Cyclase Inhibition (Can activate SRC Tyrosine Kinase)
- Gq: Phospholipase C Activation
What type of channels are involved in local anestetics (lidocaine), Antiarrhythmic Drugs (quinidine) and Druges used for treatement of epilepsy (phenytoine)?
Voltage-Gated Na+ Channels
Where are L-Type Ca2+ channels located?
Cardiac and Smooth Muscle Cells
Verapamil and Nifedipine are used to treat hypertension, arrhythmias, and ischemic heart disease. Which channel are they blocking in order to treat these diseases?
What is an adverse side effect of Verapamil?
Voltage-Gated Ca2+ Channels
Adverse Effect –> Constipation (Muscle relaxation in the gut)
Acetylcholine and Glutatmate are examples of which type of neurotransmitter?
Excitatory
GABA and Glycine are examples of which type of Neurotransmitters?
Inhibitory
Where are the two main locations of Nicotinic Acetylcholine Receptors?
- Skeletal Muscle - Responsible for depolarization of skeletal muscle fibers (Tubocurarine is an antognist drug used for nueromuscular blocks)
- Neuronal Cells - Varenicline is a partial agonist drug that is used in smoking cessation
Binding of GABA to its ion channel allows which ion to come into the cell?
Chlorine (hyperpolarization)
Steroid Hormones, Thyroid Hormones, Lipid mediators (free fatty acids), and vitamins D/A are going to bind to which type of receptor?
Nuclear Receptors
Growth hormone (somatotropin), EPO, Leptin, Interferons and Interleukins-2 to 10, 15 are going to bind to which receptor?
JAK-STAT Pathway
IGF-1, Insulin, VEGF, EGF, NGF and PDGF are going to bind to which kind of receptor?
Receptor Tyrosine Kinase
Describe the GPCR-cAMP pathway
Active G Protein - AC - cAMP - PKA - Phosphorylase Kinase - Glycogen Phosphorylase - Glycogen –> Glucose-1-Phosphate
Biogenic Amines (Ach, Epi, NE, DA, Serotonin, Histamine), Peptides/Proteins, Aminoacids, Lipids, and Nucleotides all can bind to which receptor?
GPCR
Which receptor is used as a target for inhalation/IV general anesthesia drugs, Ethanol and Valium?
GABA
SH2 domains bind to which structure?
Phosphorylated Tyrosines
