Target intelligence / Profile preview

P-glycoprotein transporter protein (P-gp)

Target
P-gp
Molecular classification
Transporter, ATP-binding cassette (ABC) transporter, MDR/TAP subfamily
01

Overview

P-glycoprotein (ABCB1) is an ATP-dependent efflux pump belonging to the ABC transporter superfamily. It plays a crucial role in transporting a wide variety of hydrophobic xenobiotics and drugs out of cells, impacting drug absorption, distribution, metabolism, and excretion. Overexpression leads to multidrug resistance in cancer, while mutations can cause specific disease phenotypes.

Other names
ABCB1MDR1Multidrug Resistance Protein 1Permeability-glycoprotein
02

Mechanism of action

ATP-dependent efflux pump expelling substrates extracellularly against concentration gradients using energy from ATP hydrolysis.

03

Biological functions

Efflux transportXenobiotic detoxificationDrug transportATP hydrolysis
04

Disease associations

Multidrug resistance in cancerColchicine resistanceInflammatory bowel disease type 13Altered pharmacokinetics
05

Safety considerations

Multidrug resistance in cancer treatmentIncreased toxicity due to loss-of-functionAltered drug efficacy/toxicity profiles
06

Interacting drugs

Dexamethasone

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