Transporters

Question 1

P-gp is what type of transporter

Answer 1

Efflux transporter

Question 2

P-gp is located on apical membrane of intestinal cells and its job is to..

Answer 2

reduce drug absorption

Question 3

What do influx transporters do

Answer 3

Enhance drug absorption

Question 4

Overexpression of an efflux transporter

Answer 4

Results in a decrease in bioavailability and systemic drug concentration

Question 5

P-gp (MDR1) located on canalicular membrane of hepatocytes

Answer 5

To move drugs out of the hepatocytes and into bile

Question 6

OCT1 (SLC22A1) on the sinusoidal membrane

Answer 6

Influx transporter that brings drugs into the hepatocytes

Question 7

In the kidney:

P-gp (MDR1) is located on the apical membrane (facing the tubule lumen) and does what

Answer 7

increases drug elimination

Question 8

P-gp in the brain

Answer 8

reduces drug penetration into the brain

Question 9

The major pharmacogenomic effects that have been presently identified are due to polymorphic expression of gene products relating to

Answer 9

drug metabolism, drug transport, and drug targets

Question 10

In patients with the T allele, expression levels of P-gp is

Answer 10

REDUCED

Question 11

Examples of target PGx

Answer 11

EGFR
HER2
HLA-B57:01
HLA-B15:02

Question 12

Erlotinib targeting EGFR

Answer 12

Erlotinib inhibits the kinase activity of EGFR, blocking signal transduction

Question 13

Trastuzumab

Answer 13

(Herceptin)

HER2