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P-glycoprotein (P-gp)-driven cancer drug resistance: biological profile, non-coding RNAs, drugs and nanomodulators

Yang Guo, Milad Ashrafizadeh, Murtaza M. Tambuwala, Jun Ren, Gorka Orive, Guiping Yu

2024Drug Discovery Today72 citationsDOIOpen Access PDF

Abstract

Drug resistance has compromised the efficacy of chemotherapy. The dysregulation of drug transporters including P-glycoprotein (P-gp) can mediate drug resistance through drug efflux. In this review, we highlight the role of P-gp in cancer drug resistance and the related molecular pathways, including phosphoinositide 3-kinase (PI3K)-Akt, phosphatase and tensin homolog (PTEN) and nuclear factor-κB (NF-κB), along with non-coding RNAs (ncRNAs). Extracellular vesicles secreted by the cells can transport ncRNAs and other proteins to change P-gp activity in cancer drug resistance. P-gp requires ATP to function, and the induction of mitochondrial dysfunction or inhibition of glutamine metabolism can impair P-gp function, thus increasing chemosensitivity. Phytochemicals, small molecules and nanoparticles have been introduced as P-gp inhibitors to increase drug sensitivity in human cancers.

Topics & Concepts

Drug resistanceP-glycoproteinPTENTensinBiologyATP-binding cassette transporterEffluxDrugMultiple drug resistancePharmacologyPI3K/AKT/mTOR pathwayCancer researchTransporterChemistryBiochemistrySignal transductionGeneGeneticsExtracellular vesicles in diseaseDrug Transport and Resistance MechanismsMicroRNA in disease regulation
P-glycoprotein (P-gp)-driven cancer drug resistance: biological profile, non-coding RNAs, drugs and nanomodulators | Litcius