Concept

Fragment-based lead discovery

Related publications (81)

Drug discovery through stem cell-based organoid models

Matthias Lütolf, Adrian Ranga, Nikolche Gjorevski

The development of new drugs is currently a long and costly process in large part due to the failure of promising drug candidates identified in initial in vitro screens to perform as intended in vivo. New approaches to drug screening are being developed wh ...

Elsevier2014

Developing the Biomolecular Screening Facility at the EPFL into the Chemical Biology Screening Platform for Switzerland

Gerardo Turcatti

The Biomolecular Screening Facility (BSF) is a multidisciplinary laboratory created in 2006 at the Ecole Polytechnique Federale de Lausanne (EPFL) to perform medium and high throughput screening in life sciences-related projects. The BSF was conceived and ...

Bentham Science Publishers2014

Seamless Integration of Dose-Response Screening and Flow Chemistry: Efficient Generation of Structure-Activity Relationship Data of β-Secretase (BACE1) Inhibitors

Horst Vogel, Michael Werner

Drug discovery is a multifaceted endeavor encompassing as its core element the generation of structure-activity relationship (SAR) data by repeated chemical synthesis and biological testing of tailored molecules. Herein, we report on the development of a f ...

Wiley-Blackwell2014

Who will develop new antibacterial agents?

Stewart Cole

The golden age of antimicrobial drug development is a distant memory, and the likelihood of there being another seems slim. In part, this is because the pharmaceutical industry, which has now adopted an unsustainable business model, abandoned the anti-infe ...

Royal Soc2014

Real-Time Monitoring of Protein Conformational Changes Using a Nano-Mechanical Sensor

Giovanni Dietler, Paolo De Los Rios, Sandor Kasas, Giovanni Longo, Dusan Vobornik, Fabrizio Benedetti, Livan Bladimir Alonso Sarduy

Proteins can switch between different conformations in response to stimuli, such as pH or temperature variations, or to the binding of ligands. Such plasticity and its kinetics can have a crucial functional role, and their characterization has taken center ...

Public Library of Science2014

Live mammalian cell arrays

Matthias Lütolf, Sebastian Maerkl, Samy Gobaa, Kristina Pan Woodruff, Luis Miguel Fidalgo Rabanera

High-content assays have the potential to drastically increase throughput in cell biology and drug discovery, but handling and culturing large libraries of cells such as primary tumor or cancer cell lines requires expensive, dedicated robotic equipment. We ...

Nature Publishing Group2013

Highly efficient production of the Alzheimer's γ-Secretase integral membrane protease complex by a multi-gene stable integration approach

Florian Maria Wurm, David Hacker, Lorène Aeschbach, Patrick Fraering, Mitko Dimitrov, Sowmya Balasubramanian

Inefficient production of membrane-embedded multi-protein complexes by conventional methods has largely prevented the generation of high-resolution structural information and the performance of high-throughput drug discovery screens for this class of prote ...

2013

Detection of Drug-Protein Interactions with an Improved Yeast Three-Hybrid System

Cindy Fellay

The identification of the targets of therapeutic drugs is one of the major challenges for pharmaceutical companies. The main target responsible for drug action is often known, but most drugs also bind other targets, either causing deleterious side effects ...

EPFL2013

Increasing the Efficiency of Ligands for FK506-Binding Protein 51 by Conformational Control

Ranganath Gopalakrishnan

The design of efficient ligands remains a key challenge in drug discovery. In the quest for lead-like ligands for the FK506-binding protein 51 (FKBP51), we designed two new classes of bicyclic sulfonamides to probe the contribution of conformational energy ...

Amer Chemical Soc2013

Cell biology: a key driver of therapeutic innovation

Oliver Hantschel

All processes associated with cellular function are likely to contribute to disease. Particularly in the cancer field, most major therapeutic innovations have originated from the elucidation of basic molecular mechanisms by academic researchers. Recent bre ...

2012

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