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Issue #3 2016



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...


Flow cytometry: breaking bottlenecks in drug discovery and development

20 September 2016 | By ,

The discovery and development of novel drug candidates is a highly complex, time-consuming and expensive process. Pharmaceutical scientists and clinicians should, therefore, reevaluate and modify the existing standard platforms and increase their uptake of robust advanced technologies such as flow cytometry to overcome the bottlenecks in these processes...


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…