Concept

Conception de médicament

Publications associées (565)

Pyridomycin bridges the NADH- and substratebinding pockets of the enoyl reductase InhA

Stewart Cole, Florence Pojer, Ruben Hartkoorn, Joao Pedro De Almeida Neres

Pyridomycin, a natural product with potent antituberculosis activity, inhibits a major drug target, the InhA enoyl reductase. Here, we unveil the co-crystal structure and unique ability of pyridomycin to block both the NADH cofactor- and lipid substrate-bi ...

Nature Publishing Group2014

The chicken chorioallantoic membrane model in biology, medicine and bioengineering

Patrycja Nowak-Sliwinska

The chicken chorioallantoic membrane (CAM) is a simple, highly vascularized extraembryonic membrane, which performs multiple functions during embryonic development, including but not restricted to gas exchange. Over the last two decades, interest in the CA ...

Springer2014

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

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

How Accurately Can We Predict the Melting Points of Drug-like Compounds?

Luc Patiny

This article contributes a highly accurate model for predicting the melting points (MPs) of medicinal chemistry compounds. The model was developed using the largest published data set, comprising more than 47k compounds. The distributions of MPs in drug-li ...

American Chemical Society2014

Cognitive Enhancers (Nootropics). Part 3: Drugs Interacting with Targets other than Receptors or Enzymes. Disease-Modifying Drugs. Update 2014

Andrea Pfeifer, Andreas Muhs

Scientists working in the field of Alzheimer's disease and, in particular, cognitive enhancers, are very productive. The review "Drugs interacting with Targets other than Receptors or Enzymes. Disease-modifying Drugs" was accepted in October 2012. In the l ...

Ios Press2014

A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR

Stewart Cole, Benoit Lechartier

A structure-guided fragment-based approach was used to target the lipophilic allosteric binding site of Mycobacterium tuberculosis EthR. This elongated channel has many hydrophobic residues lining the binding site, with few opportunities for hydrogen bondi ...

Portland Press Ltd2014

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

Assessing the essentiality of the decaprenyl-phospho-D-arabinofuranose pathway in Mycobacterium tuberculosis using conditional mutants

Stewart Cole, John McKinney, Neeraj Dhar, Claudia Sala, Ruben Hartkoorn, Gaëlle Séraphine Kolly

In Mycobacterium tuberculosis the decaprenyl-phospho-d-arabinofuranose (DPA) pathway is a validated target for the drugs ethambutol and benzothiazinones. To identify other potential drug targets in the pathway, we generated conditional knock-down mutants o ...

Wiley-Blackwell2014

Exploring Weak Ligand-Protein Interactions by Long-Lived NMR States: Improved Contrast in Fragment-Based Drug Screening

Geoffrey Bodenhausen, Daniele Mammoli, Roberto Buratto

Ligands that have an affinity for protein targets can be screened very effectively by exploiting favorable properties of long-lived states (LLS) in NMR spectroscopy. In this work, we describe the use of LLS for competitive binding experiments to measure ac ...

Wiley-Blackwell2014

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