Drug Targets

Question 1

What type of drugs are associated with inhibition of voltage gated Na channels

Answer 1

Local anesthetics

Antiarrhythmic drugs

Drugs used for tx of epilepsy

Question 2

L-type ____ channels are located on cardiac smooth muscle cells and are targets of widely used drugs, such as the antagonist ______

Answer 2

Ca; Verapamil

Question 3

2 primary excitatory NTs

Answer 3

ACh

Glutamate

Question 4

Inhibitory NTs

Answer 4

GABA

Glycine

Question 5

What NT mediates synaptic inhibition in the CNS by causing inward Cl influx and hyperpolarization, thus being used for general anesthesia, hypnotic and anti-anxiety benzodiazepines, and affects ethanol receptors?

Answer 5

GABA [to GABA-A channel]

Question 6

During RTK signaling, activation of a ras GTPase protein by growth factor requires adaptor proteins such as _____, which bind ____ and _____

Answer 6

Grb2, SH2, SH3

Question 7

During RTK signaling, activation of a Ras GTPase protein by growth factor also requires proteins regulating the activity of G-proteins, such as GEFs like ____ which activate monomeric GTPases

Answer 7

Sos

Question 8

RTK signaling pathways are drug targets in cases of cancer where the oncogene involves point mutations in ____ or ____

Answer 8

Ras; Raf

Question 9

Mineralocorticoid (aldosterone) receptor is a nuclear receptor in which _____ is produced as a result of activation of Ras; this compound is also an endogenous agonist of MR

Answer 9

Aldosterone

Question 10

End result of spironolactone, an aldosterone receptor antagonist

Answer 10

Alleviation of chronic HTN and chronic heart failure due to reduced BP and reduced cardiac workload

Question 11

Verapamil targets L-type calcium channels with the goal of treating what conditions, and what is the possible adverse effect?

Answer 11

Treats atrial and supraventricular arrhythmias, angina pectoris, and HTN

Adverse effect = constipation d/t muscle relaxation in the gut

Question 12

_____ is a drug that targets the Na/K ATPase, inhibiting it to enhance cardiac contractility

Answer 12

Digoxin

Question 13

Effects of digoxin on cardiomyocytes, GI smooth muscle, brain nuclei, and heart conduction system

Answer 13

Cardiomyocytes: causes increased contractility, thus treating CHF

GI smooth muscle: increased contractility — leads to vomiting and diarrhea

Brain nuclei: enhanced neuronal activity — leads to disorientation, confusion, visual disturbances, slowed AV conductivity, bradycardia, vomiting, and diarrhea

Conduction system: bradycardia, slowed AV conductivity

Question 14

Etoposide is a drug that inhibits topoisomerase type II — in what case would this be used, what is the effect?

Answer 14

to treat unregulated cell division in cancer

DNA damage caused by topoisomerase inhibitor leads to activation of tumor suppressor protein p53

P53 induces expression of proteins that target mitochondria to release proapoptotic proteins into cytosol, these proteins activate caspases to trigger apoptosis of a cancer cell