Target intelligence / Profile preview

P-glycoprotein 1 (P-gp)

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

Overview

P-glycoprotein 1 (P-gp) is an evolutionarily conserved transmembrane protein crucial for cellular defense against toxins but also responsible for clinically significant multidrug resistance due to its broad substrate specificity as an active efflux pump powered by ATP hydrolysis. It impacts both normal physiology—by protecting sensitive tissues—and pharmacology—by influencing how drugs are absorbed/distributed/metabolized/excreted/resisted throughout the body.

Other names
MDR1ABCB1CD243Multidrug resistance protein 1ATP-binding cassette sub-family B member 1Cluster of differentiation 243Permeability glycoprotein
02

Mechanism of action

ATP-dependent efflux; actively pumps substrates out of cells against concentration gradients.

03

Biological functions

Efflux pumpXenobiotic transportDrug transportCytokine secretionLymphocyte survivalAntigen presentationADMET regulation
04

Disease associations

Cancer (multidrug resistance)Drug-drug interactionsAltered drug bioavailability
05

Safety considerations

Multidrug resistance in cancerDrug-drug interactions due to altered pharmacokineticsVariations in drug bioavailabilityPotential for food-drug interactions
06

Interacting drugs

Many drugs are P-gp substrates or inhibitors

1 more in the full profile.

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