PK/PD in an Era of Drug Transporters

Table of Contents

PK/PD in an Era of Drug Transporters

Discovery of drug transporters

Anticancer drugs transporters : discovery

Anticancer drugs transporters : inbition by chemically-unrelated other anticancer drugs

Anticancer drug efflux inhibited by an antibiotic ...

Antifungal drugs transporters : discovery

Antifungal drug efflux

Antibiotic transporters in bacteria : 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 indeed much more than drugs ...

Why amphiphilic compounds ?

Because they are the only ones that can easily pass across membrane bilayers ...

Why should cells extrude amphiphilic compounds ?

But why drugs ?

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

Two probable mechanisms of drug transport by eucaryotic efflux pumps ...

Do efflux pumps act as vacuum cleaners ?

Two probable mechanisms of drug transport by eucaryotic efflux pumps...

Do efflux pumps act as flippases ?

Drugs and physiological substrates for transporters in eucaryotic cells

Biological significance of antibiotic transport ...

Efflux and multi / cross-resistance in pathogenic bacteria

Efflux and selection of resistance to FQ

Efflux and selection of resistance to FQ

Efflux and selection of resistance to FQ

Efflux and selection of resistance

Biological significance of antibiotic transport ...

Tissue PK : combined action of drug transporters for drug elimination / absorption

Tissue PK: combined action of drug transporters for drug elimination / absorption

Tissue PK: efflux cooperates with other mechanisms of drug clearance

Tissue PK: Efflux may also contribute to poor oral absorption

Cellular PK: ciprofloxacin efflux in macrophages

Cellular PK: ciprofloxacin efflux in macrophages

Cellular PK : handling of macrolides macrophages

Towards the future ...

They contributed to this review and/or gave us unpublished data...

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