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Issue #3 2016

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Hit-To-Lead In-Depth Focus 2016

20 September 2016 | By Drug Target Review

In this Hit-To-Lead In-Depth Focus: Hit-to-lead in drug discovery; Zebrafish early-life stages as neurological screening and detection tools...


Switching on genes regulating oxysterol synthesis – a therapeutic option?

20 September 2016 | By

Cholesterol is a ubiquitous molecule that, while essential for health, is probably best known as a risk factor for cardiovascular disease. It is also the obligate precursor for a wide range of metabolites, from steroid hormones to bile acids. Although studied for more than 100 years, recently there has been…


High-throughput calcium flux assays: luminescent versus fluorescent readout

20 September 2016 | By , , ,

In vitro high-throughput cellular target-based assays are commonly used for hit identification targeting G-protein coupled receptors (GPCR). Agonist and antagonist identification of GPCRs often relies on the screening of large collections of chemicals using miniaturised in vitro cell-based functional assays. In the panel of assays, calcium mobilisation measured by aequorin…


A picture is worth a thousand endpoints: high-content imaging in drug discovery

12 September 2016 | By , ,

Over the past few years several factors in the drug discovery industry have come together to drive an increased interest and subsequent surge in the use of high-content imaging. These include the high costs of attrition in the clinic due to lack of efficacy; increased hurdles and rising costs to…