Publications associées (41)

Development of cyclic peptides that can be administered orally to inhibit disease targets

Christian Heinis, Manuel Leonardo Merz

Cyclic peptides can bind challenging disease targets, but their oral application is hindered by digestion and absorption issues. We developed a versatile method for the synthesis and functional screening of vast numbers of synthetic cyclic peptides and ide ...
Berlin2023

Development of stimuli-responsive chemistry for tumor-targeted immunotherapy

Céline Jasmin Prange

Cancer immunotherapy is the science of boosting the immune response of patients to fight cancer. Recent advances have brought up treatments with huge success in the clinic. Patients with ad-vanced-stage cancers were long-term cured through checkpoint inhib ...
EPFL2023

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

Determination of a clinically effective evobrutinib dose: Exposure-response analyses of a phase II relapsing multiple sclerosis study

The pharmacometric analysis of the double-blind, randomized, phase II study (NCT02975349) investigating the safety and efficacy of evobrutinib, explored exposure-response relationships and suitable dosing regimens of evobrutinib for relapsing multiple scle ...
WILEY2022

In-vitro digestion of Tire and Road Wear Particles: Bioavailability of metals and Polycyclic Aromatic Hydrocarbons

Kristin Schirmer, Florian Frédéric Vincent Breider, Benoît Jean Dominique Ferrari, Thibault Béranger Masset

The potential impact of Tire and Road Wear Particles (TRWP) on aquatic organisms has recently gained attention since the occurrence of TRWP in the aquatic environment has been observed in surface water and sediments of numerous regions. Moreover, the inges ...
2021

Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism

Henning Paul-Julius Stahlberg, Dongchun Ni

ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In previously reported structures, the reaction cycle was halted by the absence of substrates or ATP, mutation of catalytic residue ...
NATURE RESEARCH2021

Towards the Development of Orally Available Peptide Therapeutics

Christian Heinis, Xudong Kong

Peptides have a number of attractive properties that make them an interesting modality for drug development, including their ability to bind challenging targets, their high target specificity, and their non-toxic metabolic products. However, a major limita ...
2021

Catalytic effects of photogenerated Fe(II) on the ligand-controlled dissolution of Iron(hydr)oxides by EDTA and DFOB

Janet Gordon Hering

Low bioavailability of iron due to poor solubility of iron(hydr)oxides limits the growth of microorganisms and plants in soils and aquatic environments. Previous studies described accelerated dissolution of iron(hydr)oxides under continuous illumination, b ...
PERGAMON-ELSEVIER SCIENCE LTD2021

Potential bioavailability of inorganic compounds from Tire and Road Wear Particles to fish in simulated gastric and intestinal fluids

Florian Frédéric Vincent Breider, Benoît Jean Dominique Ferrari, Thibault Béranger Masset

The potential impact of Tire and Road Wear Particles (TRWP) on aquatic organisms has recently gained attention since the occurrence of TRWP in the aquatic environment has been demonstrated in surface water and sediments of numerous regions. However, data r ...
2020

A reduced form of nicotinamide riboside defines a new path for NAD(+) biosynthesis and acts as an orally bioavailable NAD(+) precursor

Carlos Canto Alvarez, Richardus Houtkooper, Sofia Moco

Objective: A decay in intracellular NAD(+) levels is one of the hallmarks of physiological decline in normal tissue functions. Accordingly, dietary supplementation with NAD(+) precursors can prevent, alleviate, or even reverse multiple metabolic complicati ...
ELSEVIER2019

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