Antibiotic transporters : biology, medical issues and drug development applications

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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 ...

Author: F. Van Bambeke

Email: tulkens@facm.ucl.ac.be

Home Page: http://www.md.ucl.ac.be/facm/facm-conferences.htm