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Covalent fragment screening in cell-based phenotypic models of disease: a collaborative approach

22 June 2021 | By , , , ,

The application of chemical perturbation approaches in phenotypic models is often used to identify protein targets for therapeutic discovery. Increasingly, small molecule fragments which covalently bind to their protein targets are being used to explore the druggable proteome and the resulting fragment‑protein interactions are characterised by chemoproteomic techniques. In this…

Targeting phosphodiesterase 3A: discovery of a promising cancer therapy

22 June 2021 | By , ,

A new promising sarcoma target, phosphodiesterase 3A (PDE3A), and drugs targeting it have been identified by researchers at the University of Helsinki. Dr Katja Ivanitskiy, Dr Harri Sihto and Professor Olli Kallioniemi outline emerging evidence that indicates PDE3A protein-targeting compounds may induce sarcoma cell death by acting as a molecular…

Screening for COVID-19 drugs

22 June 2021 | By

With the COVID-19 pandemic ongoing, new therapeutic drugs to combat SARS-CoV-2 are still required. In this article, Professor Arvind Patel from the Medical Research Council (MRC) – Centre for Virus Research (CVR) at the University of Glasgow spoke with Drug Target Review’s Victoria Rees to discuss the work being done…

Why some screening hits are a PAIN

22 June 2021 | By

A major challenge during high-throughput and fragment screening is the potential for identifying ‘frequent hitters’ – compounds that affect unrelated targets. Matthew Lloyd from the University of Bath explains why these hits can arise during drug discovery and how machine learning could be the answer to identifying these compounds.

The use of biophysical methods in the hit-to-lead process

22 June 2021 | By

Optimisation of a hit towards a lead happens in a variety of ways, as a lead needs to meet various criteria such as activity, affinity to the target, selectivity, solubility, permeability or metabolic stability to become a promising candidate. A balance between in vitro profiles and pharmacokinetic attributes has to…