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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…

The potential of epigenomic medicine in cardiology

22 June 2021 | By

Advances in genomic medicine are playing an increasingly important role in the field of cardiology. Better analysis and understanding of patient genomic and epigenomic information can enable more personalised patient treatment and medical intervention. Here, Professor John Giannios considers the potential to use genomic medicine to prevent, monitor, diagnose and…

Better therapeutic antibodies by design

21 June 2021 | By

The binding specificity and high binding affinity of therapeutic antibodies makes them an ideal therapy for treating a wide range of human disorders. Advancements in antibody technologies have resulted in huge development success along with a boost in novel and improved treatment strategies. However, specific challenges and considerations are faced…

How to mix the best anti-SARS-CoV-2 cocktail

21 June 2021 | By

Neutralisation resistance generated by Spike (S) protein mutations in Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) poses a challenge to antibody therapies for COVID-19. Antibody cocktails targeting the S protein receptor binding domain (RBD) are one way to avoid viral neutralisation escape, however only certain antibody combinations are currently effective.…