Concept

Classical pharmacology

Publications associées (33)

Inhibiting Mycobacterium tuberculosis within and without

Tuberculosis remains a scourge of global health with shrinking treatment options due to the spread of drug-resistant strains of Mycobacterium tuberculosis. Intensive efforts have been made in the past 15 years to find leads for drug development so that bet ...

Royal Soc2016

Allosteric Optical Control of a Class B G-Protein-Coupled Receptor

Johannes Broichhagen

Allosteric regulation promises to open up new therapeutic avenues by increasing drug specificity at G-protein-coupled receptors (GPCRs). However, drug discovery efforts are at present hampered by an inability to precisely control the allosteric site. Herei ...

Wiley-V C H Verlag Gmbh2016

Encoded libraries of chemically modified peptides

Christian Heinis

The use of powerful technologies for generating and screening DNA-encoded protein libraries has helped drive the development of proteins as pharmaceutical ligands. However the development of peptides as pharmaceutical ligands has been more limited. Althoug ...

Elsevier2015

Next-generation antimicrobials: from chemical biology to first-in-class drugs

Paul Murima

The global emergence of multi-drug resistant bacteria invokes an urgent and imperative necessity for the identification of novel antimicrobials. The general lack of success in progressing novel chemical entities from target-based drug screens have prompted ...

Pharmaceutical Soc Korea2015

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG

Stewart Cole, Ruben Hartkoorn

To combat the emergence of drug-resistant strains of Mycobacterium tuberculosis, new antitubercular agents and novel drug targets are needed. Phenotypic screening of a library of 594 hit compounds uncovered two leads that were active against M. tuberculosi ...

Elsevier2015

Digital Holographic Imaging for Label-Free Phenotypic Profiling, Cytotoxicity, and Chloride Channels Target Screening

Gerardo Turcatti, Benjamin Rappaz, Fabien Kuttler

Cellular assays using label-free Digital Holographic Microscopy (DHM) have been previously validated for cell viability assays in a drug screening context. Our automated DHM system allows performing fast and cost-effective screening assays for a wide range ...

Springer2015

Lead selection and characterization of antitubercular compounds using the Nested Chemical Library

Stewart Cole, Ruben Hartkoorn, Edina Rita Székely

Discovering new drugs to treat tuberculosis more efficiently and to overcome multidrug resistance is a world health priority. To find novel antitubercular agents several approaches have been used in various institutions worldwide, including target-based ap ...

Elsevier2015

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1

Stewart Cole, Neeraj Dhar, Florence Pojer, Ruben Hartkoorn, Gaëlle Séraphine Kolly, Joao Pedro De Almeida Neres

Phenotypic screening of a quinoxaline library against replicating Mycobacterium tuberculosis led to the identification of lead compound Ty38c (3-((4-methoxybenzyl)amino)-6-(trifluoromethyl)quinoxaline-2-carboxylic acid). With an MIC99 and MBC of 3.1 mu M, ...

American Chemical Society2015

Screening Europe 2010: an update about the latest technologies and applications in high-throughput screening

Christoph Merten

This article reviews important presentations from the 7th Screening Europe Conference, and extracts general trends and developments. Technological advances, as well as novel applications are discussed, thus providing an overview on state-of-the-art high-th ...

2014

Establishment and Validation of Whole-Cell Based Fluorescence Assays to Identify Anti-Mycobacterial Compounds Using the Acanthamoeba castellanii - Mycobacterium marinum Host-Pathogen System

John McKinney, Hajer Ouertatani-Sakouhi, Thierry Soldati

Tuberculosis is considered to be one of the world's deadliest disease with 2 million deaths each year. The need for new antitubercular drugs is further exacerbated by the emergence of drug-resistance strains. Despite multiple recent efforts, the majority o ...

Public Library of Science2014

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