What is it about?

The kinetics of drugs binding to GPCRs has been explored in the past and linked to their physicochemical properties. This paper examines this relationship in more detail and points toward simple changes in drug properties that could improve their specificity for particular receptor subtypes.

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Why is it important?

Our findings demonstrate the potential to exploit the general structural features of receptors to which drugs bind to design more selective drugs. These structural features include overall surface charge and hydrophobicity.

Perspectives

This article was put together in lockdown following the first wave of COVID. We generated the kinetic data many years previously, so this was a great time to reflect and re-interpret the findings. As scientists, we publish a small fraction of the data we generate, so it was nice to see this project through to completion.

David Sykes
University of Nottingham

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This page is a summary of: Exploring the kinetic selectivity of drugs targeting the β 1 ‐adrenoceptor, Pharmacology Research & Perspectives, June 2022, Wiley, DOI: 10.1002/prp2.978.
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