Success Stories

Selective Optimization of Side Activities: Another Way for Drug Discovery

Journal of Medicinal Chemistry

Wermuth CG
Journal of Medicinal Chemistry - vol. 47 1303-1314 (2004)

Flow cytometry for high-throughput, high-content screening

Current Opinion in Chemical Biology

Edwards BS, Oprea T, Prossnitz ER, Sklar LA
Current Opinion in Chemical Biology - vol. 8 392-398 (2004)

Flow cytometry is a mature platform for quantitative multi-parameter measurement of cell fluorescence. Recent innovations allow up to 30-fold faster serial processing of bulk cell samples. Homogeneous discrimination of free and cell-bound fluorescent probe eliminates wash steps to streamline sample processing. Compound screening throughput may be further enhanced by multiplexing of assays on color-coded bead […]

Prednisone reduces muscle degeneration in dystrophin-deficient Caenorhabditis elegans

Neuromuscular Disorders

Gaud A, Simon JM, Witzel T, Carre-Pierrat M, Wermuth CG, Ségalat L
Neuromuscular Disorders - vol. 14 365-370 (2004)

Duchenne muscular dystrophy is a degenerative muscular disease caused by mutations in the dystrophin gene. There is no curative treatment against Duchenne muscular dystrophy. In several countries, the steroid prednisone (or analogs) is prescribed as a palliative treatment. In the model animal Caenorhabditis elegans, mutations of the dys-1 dystrophin-like gene lead to a muscular degenerative […]

Functional Electrical Stimulation and rehabilitation—an hypothesis

Medical Engineering & Physics

Rushton D
Medical Engineering & Physics - vol. 25 75-78 (2003)

Functional Electrical Stimulation (FES), used to mimic a weak or paralysed movement, sometimes is followed by a specific recovery of voluntary power in that movement. The mechanism by which this occurs is unclear, and the presumption has often been that FES may somehow promote adaptive changes in cortical connectivity. However, the unique feature of electrical […]

How to acquire new biological activities in old compounds by computer prediction

Journal of Computer-Aided Molecular Design

Poroikov VV, Filimonov DA
Journal of Computer-Aided Molecular Design - vol. 16 819-824 (2002)

Due to the directed way of testing chemical compounds’ in drug research and development many projects fail because serious adverse effects and toxicity are discovered too late, and many existing prospective activities remain unstudied. Evaluation of the general biological potential of molecules is possible using a computer program PASS that predicts more than 780 pharmacological […]

A fluorescence-based high throughput-screening assay for the SARS-CoV RNA synthesis complex

Journal of Virological Methods

Eydoux C, Fattorini V, Shannon A, Le TTN, Didier B, Canard B, Guillemot JC
Journal of Virological Methods - vol. 288 114013 (2021)

The Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV) emergence in 2003 introduced the first serious human coronavirus pathogen to an unprepared world. To control emerging viruses, existing successful anti(retro)viral therapies can inspire antiviral strategies, as conserved viral enzymes (eg., viral proteases and RNA-dependent RNA polymerases) represent targets of choice. Since 2003, much effort has been expended […]

A high-content image-based drug screen of clinical compounds against cell transmission of adenovirus

Nature Scientific Data

Georgi F, Kuttler F, Murer L, Andriasyan V, Witte R, Yakimovich A, Turcatti G, Greber UF
Nature Scientific Data - vol. 7 1-12 (2020)

Human adenoviruses (HAdVs) are fatal to immuno-suppressed individuals, but no effective anti-HAdV therapy is available. Here, we present a novel image-based high-throughput screening (HTS) platform, which scores the full viral replication cycle from virus entry to dissemination of progeny and second-round infections. We analysed 1,280 small molecular weight compounds of the Prestwick Chemical Library (PCL) […]

Bioinformatics analysis of high-throughput data to validate potential novel biomarkers and small molecule drugs for glioblastoma multiforme

Journal of International Medical Research

Qi F, Li Q, Lu X, Chen Z
Journal of International Medical Research - vol. 48 1-17 (2020)

Objective: There have been no recent improvements in the glioblastoma multiforme (GBM) outcome, with median survival remaining 15 months. Consequently, the need to identify novel biomarkers for GBM diagnosis and prognosis, and to develop targeted therapies is high. This study aimed to establish biomarkers for GBM pathogenesis and prognosis. Methods: In total, 220 overlapping differentially […]

Case studies
Use of the Prestwick Chemical Drug-Library for COVID research

In vitro screening of a FDA approved chemical library reveals potential inhibitors of SARS-CoV-2 replication.

F. Touret, M. Gilles, K. Barral, A. Nougairède, E. Decroly, X. de Lamballerie & B. Coutard
bioRxiv (2020)

Repurposing of approved drugs is a strategy that can bypass the time-consuming stages of drug development. In this study, the researchers screened the PRESTWICK CHEMICAL LIBRARY composed of 1,520 approved drugs in an infected cell-based assay. The robustness of the screen was assessed by the identification of drugs that already demonstrated in vitro antiviral effect […]

Case studies
Drug repurposing: a compound from the Prestwick Chemical Library Riboflavin Completed Phase 2 Trials for Stroke, Ischemic Treatment

Clinical validation of blood/brain glutamate grabbing in acute ischemic stroke.

A. da Silva-Candal, A. Pérez-Diaz, M. Santamaria, C. Correa-Paz, M. Rodriguez-Yanez, A. Arda, M. Perez-Mato, R. Iglesias-Rey, J. Brea, J. Azuaje, E. Sotelo, T. Sobrino, MI Loza, J. Castillo & F. Campos.
Ann. Neurol. 84 260–273 (2018)

Blood/brain-glutamate grabbing is an emerging concept in the treatment of ischemic stroke, where essentially the deleterious effects of glutamate after ischemia are ameliorated by coaxing glutamate to enter the bloodstream and thus reducing its concentration in the brain. The authors aim to demonstrate the clinical efficacy of blood glutamate grabbers in patients with stroke, and […]