Ontology highlight
ABSTRACT:
SUBMITTER: Manglik A
PROVIDER: S-EPMC3523197 | biostudies-literature | 2012 Mar
REPOSITORIES: biostudies-literature
Manglik Aashish A Kruse Andrew C AC Kobilka Tong Sun TS Thian Foon Sun FS Mathiesen Jesper M JM Sunahara Roger K RK Pardo Leonardo L Weis William I WI Kobilka Brian K BK Granier Sébastien S
Nature 20120321 7398
Opium is one of the world's oldest drugs, and its derivatives morphine and codeine are among the most used clinical drugs to relieve severe pain. These prototypical opioids produce analgesia as well as many undesirable side effects (sedation, apnoea and dependence) by binding to and activating the G-protein-coupled µ-opioid receptor (µ-OR) in the central nervous system. Here we describe the 2.8 Å crystal structure of the mouse µ-OR in complex with an irreversible morphinan antagonist. Compared t ...[more]