Medicinal Chemistry of Receptor Agonists and Antagonists

Dear Colleagues,

A wide range of receptor types, including GPCRs, nuclear receptors, cytokine receptors, hormone receptors, and pattern recognition receptors (PRRs), can serve as drug targets, depending on the specific therapeutic goal and the physiological processes involved. Receptor agonists are substances that activate or stimulate a specific receptor. Receptor antagonists, on the other hand, are substances that block or inhibit the activity of a specific receptor. Therefore, both receptor agonists and antagonists have the potential to be valuable in various clinical contexts, making them highly sought after worldwide. In general, receptor agonists and antagonists typically share an overlapping binding region. Therefore, it is of paramount importance to elucidate the principles behind ligand-induced agonism and antagonism through rational medicinal chemistry approaches, subsequently enabling the transformation of ligands between agonistic and antagonistic effects via structural modifications. This Special Issue aims to provide a forum for the dissemination of the latest advancements in the medicinal chemistry and pharmacology of receptor agonists and antagonists.

Dr. Chong Qin
Guest Editor

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• receptor agonists
• receptor antagonists
• GPCR
• nuclear receptors
• hormone receptors
• cytokine receptors