Biased activation of G-protein-coupled receptors (GPCRs) is shifting drug discovery efforts and appears promising for the development of safer drugs. The most effective analgesics to treat acute pain are agonists of the mu-opioid receptor (m-OR), a member of the GPCR superfamily. However, their therapeutic use requires close medical monitoring to diminish the risk of severe adverse effects. The G-protein-biased agonists of m-ORs have shown safer therapeutic profiles than non-biased ligands. In this talk, we will present the analysis of the chemical space covered by opioid ligands, a fingerprint codification of biased agonisim, and strategies for the modification of the pharmacological properties.

Crafting opiates: Learning from the opioid chemspace and incorporating a molecular spark

Fall 2022 abstracts, posters, and presentations will launch in mid-September.

ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.