Chapter 5 ABC Transporters

ABC gene and what it does

ABC1

Codes for P-glycoprotein aka PGY1 aka MDR1

P-glycoprotein

Helps to form protective barrier against absorption of xenobiotics in tissues with excretory or protective function

ABCB1 polymorphism

Polymorphism affecting antidepressants and opioid analgesics

Rs9282564

Associated with opioid induced respiratory depression (higher risk if children have this)

MRP1

Multidrug resistance associated protein (MRP) with greatest significance in clinical anticancer drug resistance

ABCC1

Confers resistance to anthracyclines and vinca alkaloids

ABCC2

Transports products of phase 2 metabolism from hepatic cells into canaliculi and then to bile for excretion

ABCC6

Mutations in this ABC gene associated with pseudoxanthoma elasticum (mineralization of elastic fibers

ABCC11 (MRP8)

Efflux transporter for ANIONIC LIPOphilic compounds

Confers resistance to antiviral and anticancer agents

ABCG2

ABC that is very important in limiting bioavailability of certain drugs, concentrating drugs in breast milk, and protecting fetus from drugs in maternal circulation

Considered one of the most important ABC transporters mediating multidrug resistance in cancer cells