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Screening In-Depth Focus 2019

7 June 2019 | By

This in-depth focus discusses screening and the uses of phenotypic profiling in drug discovery. Also examined is the role that CRISPR/Cas9 gene editing and native mass spectrometry play.

Imaging In-Depth Focus 2019

6 June 2019 | By

In this in-depth focus, the challenges of imaging are explored including how to develop high-resolution images. Also discussed are new imaging technologies to aid drug discovery.

Phenotypic profiling in drug discovery

5 June 2019 | By , ,

Image-based phenotypic profiling of small molecules has been used for identification and characterisation of small molecules in drug discovery and can provide important insights into their mechanisms of action (MOA). This article discusses the use of phenotypic profiling in drug discovery and how machine-learning algorithms could help improve objectivity, processing…

Drug Target Review – Issue 2 2019

5 June 2019 | By

In this issue: novel approaches to produce radiolabelled antibodies, the use of CRISPR/Cas9 to accelerate the development of targeted therapies and utilisation of stem cells to study the effects of cannabis on neuronal development.

AI-driven automated chemistry as a tool to accelerate drug discovery

15 May 2019 | By

Typically, early drug discovery campaigns start with the screening of chemical libraries to identify candidate chemotypes modulating a particular target and/or phenotype. Success of the primary screening depends on multiple factors related to both biology and chemistry. These include the target’s druggability, sensitivity and specificity of assay system, composition and…

Squaring the circle – cancer vaccines

8 May 2019 | By

By the 1890s William B. Coley had injected streptococcal organisms in patients with solid tumours (“Coley’s Toxins”) to activate the immune system. Coley (1862-1936) was an American bone surgeon and pioneer of cancer immunotherapy. He was convinced that post-surgical infections had helped patients to recover better from their cancer by…

Transforming drug discovery, development and delivery with flow chemistry

11 April 2019 | By ,

Flow chemistry is on the rise thanks to the commercial availability of benchtop continuous flow systems that has driven widespread adoption of the technique across a broad range of applications in both academia and industry. In particular, flow chemistry is delivering significant benefits in the area of drug discovery and…

The importance of characterising chemical starting points of drugs using appropriate in vitro ADME-toxicity assays

21 March 2019 | By ,

Over the past 30 years, one strategy the pharmaceutical industry has adopted in the drug discovery process has been to “fail early, fail often”.1,2 As most molecules in the early stages of drug discovery will have sub-optimal characteristics, significant modification is necessary to improve their properties.