Publications associées à Towards the Development of Orally Available Peptide Therapeutics

Cyclic Peptides for Drug Development

Christian Heinis, Xinjian Ji, Alexander Lund Nielsen

Cyclic peptides are fascinating molecules abundantly found in nature and exploited as molecular format for drug development as well as other applications, ranging from research tools to food additives. Advances in peptide technologies made over many years ...

Wiley-VCH Verlag GmbH2024

Computational drug development for membrane protein targets

Henning Paul-Julius Stahlberg, Pierre Vogel, Shuguang Yuan, Dongchun Ni, Babatunde Edukpe Ekundayo

The application of computational biology in drug development for membrane protein targets has experienced a boost from recent developments in deep learning-driven structure prediction, increased speed and resolution of structure elucidation, machine learni ...

2024

Deconvolution of ex-vivo drug screening data and bulk tissue expression predicts the abundance and viability of cancer cell subpopulations

Alexandre Coudray

Ex-vivo drug sensitivity screening (DSS) allows the prediction of cancer treatment effectiveness in a personalized fashion. However, it only provides a readout on mixtures of cells, potentially occulting important information on clinically relevant cell su ...

EPFL2023

The predictive capacity of in vitro preclinical models to evaluate drugs for the treatment of retinoblastoma

Paul Joseph Dyson, Irina Sinenko, Roland Christopher Turnell-Ritson

Retinoblastoma is a rare childhood cancer of the eye. Of the small number of drugs are used to treat retinoblastoma, all have been repurposed from drugs developed for other conditions. In order to find drugs or drug combinations better suited to the improv ...

ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD2023

Optimised three-dimensional in vitro retinoblastoma models tailored for drug discovery and clinical translatability

Irina Sinenko

Retinoblastoma, while relatively rare, stands as the most prevalent intraocular cancer. In Switzerland, the survival rate approaches 100%, but it drops to less than 50% in low-income countries. The current treatment options for retinoblastoma rely on a lim ...

EPFL2023

Alchemical analysis of FDA approved drugs

Jean-Louis Reymond, Philippe Schwaller, Markus Orsi, Daniel Probst

Chemical space maps help visualize similarities within molecular sets. However, there are many different molecular similarity measures resulting in a confusing number of possible comparisons. To overcome this limitation, we exploit the fact that tools desi ...

2023

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

Repurposed drug combination via high-throughput screening and dual drug delivery system development for the treatment of retinoblastoma

Po-Jen Tseng

The goal of retinoblastoma (RB) treatment is to save the child's life, eyes and functional vision, with that order of priority. The management of RB is complex and involves strategically chosen methods of surgical enucleation, external beam radiotherapy, i ...

EPFL2022

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

Gerardo Turcatti, Fabien Kuttler, Liliane Yang, Michael Bauer

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

Combi-seq for multiplexed transcriptome-based profiling of drug combinations using deterministic barcoding in single-cell droplets

Ngoc Hien Du, Christoph Merten

Anti-cancer therapies often exhibit only short-term effects. Tumors typically develop drug resistance causing relapses that might be tackled with drug combinations. Identification of the right combination is challenging and would benefit from high-content, ...

Nature Research2022

In-Cell Quantification of Drugs by Magic-Angle Spinning Dynamic Nuclear Polarization NMR

David Lyndon Emsley, Pierrick Berruyer, Andrea Bertarello

The determination of intracellular drug concentrations can provide a better understanding of the drug function and efficacy. Ideally, this should be performed nondestructively, with no modification of either the drug or the target, and with the capability ...

AMER CHEMICAL SOC2022

Laser-induced liquid micro-jets for drug delivery

Jan Krizek

Jet injection devices have been studied and developed for transdermal drug delivery to avoid the use of needles. Such contact-less devices provide several advantages such as better dose control, lateral and depth localisation, lower collateral damage than ...

EPFL2021

Harnessing the Membrane Translocation Properties of AB Toxins for Therapeutic Applications

Françoise Gisou van der Goot Grunberg, Oksana Andrei Sergeeva

Over the last few decades, proteins and peptides have become increasingly more common as FDA-approved drugs, despite their inefficient delivery due to their inability to cross the plasma membrane. In this context, bacterial two-component systems, termed AB ...

2021

Fabrication of micrometer-sized drops as templates for particles

Mathias Steinacher

Drops are omnipresent in our daily life for example in the form of rain drops or as oil drops in a salad dressing. On a technological basis, drops can be used to conduct chemical or biological reactions. These drops often serve as templates to produce mate ...

EPFL2021

Therapeutic approaches against coronaviruses acute respiratory syndrome

Francesco Stellacci, Camilla Servidio

Coronaviruses represent global health threat. In this century, they have already caused two epidemics and one serious pandemic. Although, at present, there are no approved drugs and therapies for the treatment and prevention of human coronaviruses, several ...

JOHN WILEY & SONS LTD2021

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

De novo development of proteolytically resistant therapeutic peptides for oral administration

Christian Heinis, Florence Pojer, Luciano Andres Abriata, Xudong Kong, Kaycie Marie Butler, Vanessa Carle, Jun Moriya

The oral administration of peptide drugs is hampered by their metabolic instability and limited intestinal uptake. Here, we describe a method for the generation of small target-specific peptides (less than 1,600 Da in size) that resist gastrointestinal pro ...

2020

A Drug Release Mechanism Controlled by Hydrophobic/Hydrophilic Balance of the Matrix. Theoretical and Experimental Perspectives

Maria-Alexandra Paun

Controlled drug release is a promising pathway of biomedicine, meant to suppress side effects with the aim of increasing patient's comfort. A route to achieve this goal represents the encapsulation of drugs into matrixes, capable to develop physical forces ...

REVISTA CHIMIE SRL2020

Experimental And Theoretical Insight Into Formulations Based On Poly(Vinyl Alcohol Boric Acid) And Diclofenac Sodium Salt

Maria-Alexandra Paun

A series of three formulations were prepared in view of experimental and theoretical investigation of their drug release potential. The morphology of the film formulations, in terms of distribution of drug into the polymeric matrix and the nature of the dr ...

UNIV POLITEHNICA BUCHAREST, SCI BULL2020

3D Printed Micro-Scaffolds Loaded by Inkjet Printing With in-Precise Amount of Drug

Jürgen Brugger, Christopher Chi Wai Tse, Jongmoon Jang, Fengyi Zheng

We propose a novel combination of two-photon polymerization (2PP) three-dimensional (3D) micro-manufacturing with drop-on-demand inkjet printing (DOD IJP) to fabricate 3D microporous scaffolds embedded with minute quantities of releasable drug. We designed ...

IEEE2020