The permeability of biological membranes is one of the most important determinants of the
pharmacokinetic processes of a drug. Although it is often accepted that many drug …

With the discovery of P-glycoprotein (P-gp), it became evident that ABC-transporters play a
vital role in bioavailability and toxicity of drugs. They prevent intracellular accumulation of …

Benzodiazepines exert their anxiolytic, anticonvulsant, muscle-relaxant and sedative-hypnotic
properties by allosterically enhancing the action of GABA at GABA A receptors via their …

Highlights • A public–private partnership targets drug-binding kinetics in a multilevel
approach. • New experimental approaches for measuring drug residence time are presented. • …

Evidence supporting the action of passive diffusion and carrier-mediated (CM) transport in
drug bioavailability and disposition is discussed to refute the recently proposed theory that …

In silico toxicology is an emerging field. It gains increasing importance as research is aiming
to decrease the use of animal experiments as suggested in the 3R principles by Russell …

Recently, it has been proposed that drug permeation is essentially carrier-mediated only and
that passive lipoidal diffusion is negligible. This opposes the prevailing hypothesis of drug …

Protein degradation is an emerging therapeutic strategy with a unique molecular pharmacology
that enables the disruption of all functions associated with a target. This is particularly …

The serotonin transporter (SERT) terminates neurotransmission by removing serotonin from
the synaptic cleft. In addition, it is the site of action of antidepressants (which block the …

P-glycoprotein (P-gp) is an energy-dependent multidrug efflux pump conferring resistance
to cancer chemotherapy. Characterization of the mechanism of drug transport at a molecular …