Phenotypic Screening

Dear Colleagues,

Phenotypic screening and more broadly phenotypic drug discovery (PDD) rely on methods where the molecular mechanism is not known or assumed and uses empirical lead generation to deliver novel drug candidates in the clinic. Though target-based approaches, supported by the rapid progress in genetics and molecular biology, have dominated drug discovery in the past 30 years, there is recently a resurgence of PDD. The relative simplicity of target-based approaches facilitated testing of increasing numbers of compounds, initially thought of as increasing diversity and furthering the odds of successful drug discovery. However, a disconnect between in vitro and in vivo systems was often observed, as a result of stirring away from physiologically relevant conditions that cease to accurately simulate disease. PDD, on the other hand, is more costly and slow in the early stages, requiring rigorous validation and/or target identification, but with a better understanding of the risks and challenges, it can be a powerful tool leading to increased probabilty of success for drug candidates, but also to the identification of novel drug targets that can be used alone or in combination with existing therapeutics.

The present Special Issue is aimed at covering improvements in library design, screening, assay cascade, and chemoinformatics tools that expedite modern PDD, presenting successful medicinal chemistry efforts in PDD, and further target identification campaigns that originated from PDD. We look forward to receiving these and other relevant contributions.

Dr. Maria Chatzopoulou
Prof. Dr. Angela Russell
Guest Editors

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