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Screening In-Depth Focus 2014

7 May 2014 | By Kenji Schorpp, Christophe Antczak, Balajee Somalinga, Hakim Djaballah

In this Screening In-Depth Focus: Kenji Schorpp looks at targeting the ubiquitin-proteasome system, and experts from Memorial Sloan-Kettering Cancer Center discuss a high content assay opportunity to measure cellular stress response using heat shock proteins...

Building GPCR screening cascades for lead generation

6 May 2014 | By , , ,

Although this target class is already heavily investigated, there are still a significant number of opportunities for discovery of novel drugs targeting additional GPCRs. In this review, scientists from AstraZeneca R&D discuss the general build-up of GPCR screening cascades for discovery of chemical leads that can be further developed into…

Oncology biomarkers in clinical practice – a new horizon

4 May 2014 | By , ,

The ability to individualise a patient’s care has become a particularly pressing issue in the field of cancer therapeutics as there is a growing recognition that both the global incidence of cancer is steadily rising and the associated costs in terms of treatment and lost productivity are ever increasing. Advances…

Marine Drug Discovery: Realising the potential of therapeutics from marine sources – lessons from Big Pharma

3 May 2014 | By

Oceans cover 70 per cent of planet Earth and it is only in the 20th century that organisms from this environment began to be assessed for their potential to provide new drugs. A new marine derived pharmaceutical pipeline has started flowing, delivering new chemical entities with unique modes of action…

Molecular Target Validation in preclinical drug discovery

2 May 2014 | By , , ,

Preclinical drug target validation has the aim to increase confidence in a particular drug target. The process proves the initial hypothesis that a particular molecular target is key or even causative for pathogenic or symptomatic mechanisms in a disease. Several success factors seem to be of particular importance for the…

Nuclear Magnetic Resonance as a tool for chemokine inhibitor discovery

1 May 2014 | By

Chemokines orchestrate leukocyte trafficking in the immune system, but unregulated or inappropriate chemokine activity plays a key role in many inflammatory, allergic and autoimmune diseases as well as metastatic tumour progression. The chemokine network is comprised of ~50 distinct ligands that specifically bind and activate a family of 20 G…