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Screening 2018

 

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Leveraging the power of HTS in the new and rapidly evolving collaborative drug discovery landscape

1 December 2018 | By ,

Over the last five years drug discovery has undergone a rapid evolution from a closed and proprietary endeavour to an open and collaborative process. Large and small pharma now openly collaborate with each other and the wider academic world to leverage their collective depth of knowledge to increase the chances…

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A high-throughput approach for measuring intracellular ATP levels to access compound-mediated cellular toxicity

30 November 2018 | By , , ,

Many drugs fail in clinical trials due to toxicity-related issues; therefore, drug-mediated cellular toxicity should be determined at an early stage in the drug discovery value chain. There are many assay systems that can be utilised to measure cellular toxicity. In this article we demonstrate that intracellular ATP concentrations are…

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The role of drug transporters in phenotypic screening

27 November 2018 | By , , ,

The relative failure of molecular target-based drug discovery has led to a return to phenotypic screening. Targets that are intracellular necessitate their drug ligands to pass through plasma membranes, where the protein:lipid ratio is often 3:1 by mass and at least 1:1 by area. The widespread view that most of…

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Cancer drug screening: the historical perspective

20 July 2018 | By , , , ,

Chemotherapy with cytotoxic and growth inhibitory drugs have played an important role in cancer therapy, used either alone or in combination with other treatment modalities such as surgery, radiation or biological therapy. Chemotherapy, in most instances, was the only alternative treatment for metastatic cancer – mainly given as drug combinations...