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Issue #4 2018

 

Beyond ‘simple’ biology – turning organoids, spheroids, and 3D tissue models into physiologically relevant high-content assays for drug discovery

11 December 2018 | By

Drug discovery is still hampered by the routine use of cell-based models that often fail to recapitulate the truly relevant biological complexity of the corresponding disease. Just moving from two- (2D) towards three-dimensional (3D) cell culture model systems like spheroids and organoids is not enough to generate truly representative and…

New frontiers in G protein-coupled receptor drug discovery

10 December 2018 | By

G protein-coupled receptors (GPCRs) are seven transmembrane spanning proteins that mediate the physiological responses to a broad array of stimuli, including photons, biogenic amines, peptides and large proteins. They represent the target of approximately one-third of all approved drugs,1 yet paradoxically remain a relatively under-exploited protein class.

Webinar highlights: Integrated fragment based approach reveals enzymatic inhibitors with potential therapeutic application

10 December 2018 | By

This webinar, held on 25 October 2018, presented the results from integrated fragment-based approaches for Indoleamine 2,3 dioxygenase 1 (IDO1), an enzyme widely recognised as a drug target for the development of immunotherapeutic small molecules in oncology, unveiling the first ligands able to modulate non-catalytic signalling.

Omics-informed drug target discovery in combating emerging infectious diseases  

7 December 2018 | By

The catastrophic consequences of ever-increasing rates of death from infectious diseases demands new experimental strategies for drug target selection and drug design. Over the last decade, the pharmaceutical industry has been wounded by several issues including failure of drug-development programmes, burgeoning cost of drug development, increasing regulatory control, lack of…

Expert view: Three-dimensional cell cultures as predictive tools in early drug discovery

6 December 2018 | By

Three-dimensional cell cultures (spheroids, organoids) are becoming widely used as a new predictive tool in early drug discovery. The use of 3D cell cultures is believed to provide a more physiologically relevant response than monolayer (2D) cell cultures because they closely mimic the extracellular matrix and cell-cell interactions that occur…

PAINS management: an open source model to eliminate nuisance compounds

4 December 2018 | By

High-throughput screening (HTS) technologies have enabled the routine testing of millions of compounds towards the identification of novel ‘hit’ molecules for therapeutic targets. Oftentimes in this drug discovery process, however, compounds that show promising activity in primary screens show no activity during subsequent hit qualification or progression efforts.

Application Notes supplement 2018

4 December 2018 | By

Researchers are always looking more effective and efficient ways of making their work more successful. In this supplement, some of our commercial partners share their data, detailing the application of their technology.