… Only compounds with low passive permeation show significant active transport expressed
by the R GF ratio (apical (a) to basolateral (b) transport rate ratio (inhibited/non inhibited)). …

… Very recently, the hitherto largest data set for BCRP has been compiled by Montanari and
Ecker, and includes 978 unique compounds extracted from 47 studies [43]. Subsequently, the …

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

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

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 reactions, lasting between 0.5 and 60 min, were terminated by rapid washing with ice-cold
buffer and collected onto glass fiber filters (Whatman GF/B) that were dissolved in …

… In-gel digestions were performed according to the procedure described by Ecker et al. (2002…
as a function of this amino acid position as described in Ecker et al. (2004). The resulting …