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Concept

First pass effect

Related publications (6)

De novo developed small cyclic peptides that are orally available

Manuel Leonardo Merz

Cyclic peptides are ring-shaped molecules that emerged as a promising class of therapeutics. While it is often difficult to find small molecule binders for challenging disease targets, cyclic peptides can bind to featureless surfaces or inhibit protein-pro ...

EPFL2022

NICEdrug.ch, a workflow for rational drug design and systems-level analysis of drug metabolism

Vassily Hatzimanikatis, Noushin Hadadi, Jasmin Maria Hafner, Anush Chiappino-Pepe, Homa Mohammadi Peyhani

The discovery of a drug requires over a decade of intensive research and financial investments – and still has a high risk of failure. To reduce this burden, we developed the NICEdrug.ch resource, which incorporates 250,000 bioactive molecules, and studied ...

2021

Electrostatic spray ionization from 384-well microtiter plates for mass spectrometry analysis based enzyme assay and drug metabolism screening

Hubert Girault, Liang Qiao, Tzu-En Lin, Elena Tobolkina, Xiaoqin Zhong

We have realized the direct ionization of samples from wells of microtiter plates under atmospheric conditions for mass spectrometry analysis without any liquid delivery system or any additional interface. The microtiter plate is a commercially available 3 ...

American Chemical Society2017

Abcb4 acts as multixenobiotic transporter and active barrier against chemical uptake in zebrafish (Danio rerio) embryos

Kristin Schirmer

Background: In mammals, ABCB1 constitutes a cellular "first line of defense" against a wide array of chemicals and drugs conferring cellular multidrug or multixenobiotic resistance (MDR/MXR). We tested the hypothesis that an ABCB1 ortholog serves as protec ...

Biomed Central Ltd2013

Dynamical Spot Queries to Improve Specificity in P450s based Multi-Drugs Monitoring

Giovanni De Micheli, Sandro Carrara, Andrea Cavallini, Abhishek Garg

Personalized therapy requires accurate and frequent monitoring of drugs metabolic response in living organisms during drug treatments. In case of high risk side effects, e.g. therapies with interfering anti-cancer molecules cocktails, direct monitoring of ...

2009

Inducibility of Drug-metabolizing Enzymes by Xenobiotics in Mice with Liver-specific Knockout of Ctnnb1

Jörg Hülsken

Basal as well as xenobiotic-induced expression of the main enzymes from phase I and phase II of drug metabolism is confined to the perivenous areas of the mammalian liver lobule. Whereas signal transduction pathways that govern xenobiotic-induced expressio ...

2009