ICPP 3 Organic Anion And Cation Transporters - Importance In Drug Metabolism

Question 1

What type of transporters are solute carrier transport proteins?

Answer 1

Secondary active or facilitated transporters

Question 2

What are the two main subfamilies of SLC22?

Answer 2

Organic anion transporters
Organic cation transporters

Question 3

Where are organic anion transports common?

Answer 3

Cell types that have barriers between fluid compartments

Commonly localised to epithelial cells

Question 4

What is important for antibiotic transport?

Answer 4

Organic anion transporters

Question 5

What do OATs bind to?

Answer 5

Anionic (negatively charged) substrates

Question 6

What do OCTs bind to?

Answer 6

Cationic (positively charged) substrates

Question 7

What are required for drugs to reach their target and why?

Answer 7

• Many drugs are hydrophilic/charged
• Depend on carrier mediated transport for absorption, distribution + elimination at each membrane boundary from site of admission

Question 8

Outline metformin transport by OCTs

Answer 8

• OCT1 transports metformin into hepatocytes
• Decreases hepatic glucose production

Question 9

What is metformin used for?

Answer 9

Treatment of type 2 diabetes

Question 10

Explain the toxicity related to cisplatin

Answer 10

Poor substrate of MATE1 or MATE2-K
Cisplatin accumulates in cells&raquo_space; cell death