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Target intelligence / Profile preview
ATP-binding cassette subfamily B member 1 (ABCB1)
- Target
- ABCB1
- Molecular classification
- Transporter, ATP-binding cassette transporter, ABC transporter
01
Overview
ABCB1 is an ATP-dependent efflux pump responsible for transporting a wide variety of drugs and other substances out of cells. It plays a critical role in multidrug resistance, particularly in cancer, and impacts the pharmacokinetics of many clinically used drugs. It is highly expressed at blood-organ barriers where it protects tissues from toxic substances. Genetic variants influence individual drug responses, which can lead to drug toxicity or therapeutic failure. The protein consists of two pseudosymmetric halves, each containing a transmembrane domain (TMD) and a nucleotide-binding domain (NBD). The TMDs form a central drug-binding pocket surrounded by 12 transmembrane helices. It belongs to one of seven distinct subfamilies within the large superfamily of human ATP-binding cassette (ABC) transporters.
- Other names
- MDR1P-glycoprotein
02
Mechanism of action
ATP hydrolysis-driven active transport via alternating access mechanism
03
Biological functions
Efflux pumpDrug transportXenobiotic transportProtection of tissues from toxic substances
04
Disease associations
Multidrug resistance in cancerColchicine resistanceInflammatory bowel disease
05
Safety considerations
Drug toxicity due to altered pharmacokineticsTherapeutic failure in cancer treatment due to multidrug resistanceGenetic variants influence individual drug responses
06
Interacting drugs
Chemotherapeutic agents (ABCB1 substrates)
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