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Pleiotropic drug resistance protein 5 (Pdr5)
- Target
- Pdr5
- Molecular classification
- Transporter, ABC transporter family (ATP-binding cassette transporter), PDR subfamily (Pleiotropic Drug Resistance subfamily)
01
Overview
Pleiotropic drug resistance protein 5 (Pdr5) is a yeast ABC transporter responsible for the active efflux of a wide variety of structurally diverse, weakly charged organic compounds, particularly antifungal drugs. It functions via ATP hydrolysis, undergoing conformational changes to move substrates from the cytoplasm to the extracellular space. Pdr5 is highly abundant in yeast cells (~42,000 copies/cell) and is a major determinant of multidrug resistance, contributing to the organism’s survival under antifungal stress. Its molecular structure, determined by cryo-EM, reveals a complex nucleotide-sensing mechanism and asymmetric action in drug translocation, making it a prime target for research into combating drug resistance in fungi
- Other names
- Pdr5PDR5Pleiotropic ABC efflux transporterMultidrug transporter Pdr5p
02
Mechanism of action
ATP-driven drug efflux (hydrolyzes ATP to power substrate translocation); Mechanically pumps drugs from cytoplasm to the cell exterior via an amphipathic channel; Target for inhibition (e.g., FK506 inhibits wild-type Pdr5-mediated resistance)
03
Biological functions
Drug effluxDetoxificationCellular defense against toxic compoundsContribution to pleiotropic drug resistance
04
Disease associations
Infection (fungal resistance to antifungals in both yeast and pathogenic fungi)Other (model for understanding multidrug resistance mechanisms)
05
Safety considerations
Drug resistance (therapeutic challenge: reduces efficacy of antifungals)Substrate-dependent variability (different mutants show varying drug susceptibilities)
06
Interacting drugs
Rhodamine 6G
5 more in the full profile.
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