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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.…

Drug Target Review – Issue 2 2021

14 June 2021 | By

This issue includes articles on novel AAV vectors to deliver ocular gene therapy, how phenotypic models of disease are being used in covalent fragment screening and the challenges and opportunities presented by automation in the life sciences. Also in this issue are features on stem cells, antibodies and hit-to-lead.