Target intelligence / Profile preview

ATP-binding cassette sub-family B member 1 mRNA (MDR1 mRNA)

Target
MDR1 mRNA
Molecular classification
Messenger RNA, ATP-binding cassette transporter family
01

Overview

MDR1 mRNA, transcribed from the ABCB1 gene (NCBI Gene ID: 5243), is the genetic template for P-glycoprotein (P-gp), a member of the ATP-binding cassette (ABC) transporter family (UniProt: P08183). This mRNA is a primary driver of multidrug resistance (MDR) in cancer, as its overexpression leads to an abundance of P-gp, which actively effluxes a wide variety of chemotherapeutic agents from the cytoplasm (PubMed: 25653465). Beyond its role in malignancy, MDR1 mRNA is expressed in normal tissues such as the liver, kidneys, and the endothelial cells of the blood-brain barrier (BBB), where it serves a protective role by limiting the entry of toxins into sensitive organs (PubMed: 11470988). Therapeutic targeting of MDR1 mRNA using small interfering RNAs (siRNAs) or antisense oligonucleotides (ASOs) aims to silence the production of P-gp, thereby restoring the efficacy of chemotherapy in resistant tumors (PubMed: 30234144). However, such interventions pose significant safety risks, including the potential for increased systemic toxicity of co-administered drugs and the compromise of the BBB, which can lead to neurotoxicity. Monitoring MDR1 mRNA levels via RT-qPCR is often used as a biomarker to predict or evaluate drug resistance in clinical settings.

Other names
ABCB1 mRNAP-glycoprotein 1 mRNAP-gp mRNACD243 mRNA
02

Mechanism of action

RNA interference (RNAi) or antisense-mediated mRNA degradation and translational repression.

03

Biological functions

Protein translationXenobiotic transportDrug effluxMultidrug resistance
04

Disease associations

CancerMultidrug resistanceRefractory epilepsyInflammatory bowel disease
05

Safety considerations

Increased systemic toxicity of co-administered drugsBlood-brain barrier (BBB) disruptionOff-target RNA silencing
06

Interacting drugs

siRNA (experimental)

1 more in the full profile.

07

Biomarkers

MDR1 mRNA expression levels (RT-qPCR)P-glycoprotein (P-gp) protein levelsRhodamine 123 efflux activity

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