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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 ...

2023

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

Mitchell David Anderson

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

Identification of broad anti-coronavirus chemical agents for repurposing against SARS-CoV-2 and variants of concern

Gerardo Turcatti, Fabien Kuttler, Michael Bauer, Liliane Yang

Endemic human coronaviruses (hCoVs) 229E and OC43 cause respiratory disease with recurrent infections, while severe acute respiratory syndrome (SARS)-CoV-2 spreads across the world with impact on health and societies. Here, we report an image-based multicy ...

2022

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

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 ...

2019

Optimized Sampling Rate for Voltammetry-Based Electrochemical Sensing in Wearable and IoT Applications

Sandro Carrara, Danilo Demarchi, Simone Aiassa

The recent advancements in electrochemical measurements are guiding the development of new platforms for in situ point-of-care monitoring of human-metabolite, markers, and drugs. Despite this, the application of voltammetry-based sensing (VBS) techniques i ...

2019

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

Mitchell David Anderson

WILEY2022

De novo developed small cyclic peptides that are orally available

Manuel Leonardo Merz

EPFL2022

Towards the Development of Orally Available Peptide Therapeutics

Christian Heinis, Xudong Kong

2021

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

2019

Optimized Sampling Rate for Voltammetry-Based Electrochemical Sensing in Wearable and IoT Applications

Sandro Carrara, Danilo Demarchi, Simone Aiassa

2019