Table of Contents
Antibiotic transporters :biology, medical issues and drug development applications
Discovery of drug transporters
Anticancer drugs transporters : discovery
Anticancer drugs transporters : inbition by chemically-unrelated other anticancer drugs
Main anticancer drugs transporter
Inhibition by an unrelated drug …
Anticancer drugs transporters can be inhibited by an antibiotic ...
Antifungal drugs transporters : discovery
Antifungal drug efflux
Antibiotic transporters : discovery
Antibiotic transporters : discovery
Why drug transporters ?
There is much more than drugs ...
Inventory of transporters in the complete genomes of S. cerevisiae and E. coli
There is much more than drugs ...
Why amphiphilic compounds ?
Why amphiphilic compounds ?
Why amphiphilic compounds ?
Transporters - data bases
Most frequent antibiotic-pumps in procaryotes (1/2)
Most frequent antibiotic-pumps in procaryotes (2/2)
Most frequent antibiotic-pumps in eucaryotes (1/2)
Most frequent antibiotic-pumps in eucaryotes (2/2)
Antibiotic classes recognized by efflux pumps in different types of organisms
Antibiotics are amphiphilic substrates :
Antibiotics are amphiphilic substrates :
Mechanisms of drug transport ...
Do efflux pumps act as pores ?
Do efflux pumps act as vacuum cleaners ?
Do efflux pumps act as flippases ?
Biological significance of antibiotic transport ...
Efflux and resistance in pathogenic bacteria
Efflux and resistance in pathogenic bacteria
Efflux cooperates with other mechanisms of bacterial resistance
Efflux cooperates with other mechanisms of resistance
Efflux and selection of resistance to FQ
Efflux and selection of resistance
Biological significance of antibiotic transport ...
Transporters involved in the efflux of antibiotics from eucaryotic cells
Combined action of drug transporters for drug elimination / absorption
Combined action of drug transporters for drug elimination / absorption
Efflux cooperates with other mechanisms of drug clearance
Efflux may also contribute to poor oral absorption
Evidencing active efflux : experimental strategy
Evidencing active efflux : experimental strategy
Evidencing active efflux : experimental strategy
In search for efflux pumps to fluoroquinolones in macrophages
Cellular pharmacokinetics [1 of 2]
Cellular pharmacokinetics [2 of 2]
Characterization of the transporter(s) [1 of 3]
Characterization of the transporter(s) [2 of 3]
Which type of efflux transporter might be involved ?
Characterization of the transporter(s) [2 of 3]
Probenecid - resistant macrophages [1 of 2]
Wild-type versus probenecid - resistant macrophages [2 of 2]
Therapeutic perspectives
New derivatives of antibiotics with reduced affinity for transporters
New derivatives of antibiotics with reduced affinity for transporters
New derivatives of antibiotics with reduced affinity for transporters
New derivatives of antibiotics with reduced affinity for transporters
New derivatives of antibiotics with reduced affinity for transporters
New derivatives of antibiotics with reduced affinity for transporters
Inhibitors of efflux pumps as adjuvant therapy
Inhibitors of efflux pumps ...
Inhibitors of efflux pumps ...
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