Opioid receptors (ORs) are among the best studied G protein-coupled receptors due to their involvement in neurological disorders and important role in pain treatment. Contrary to the classical monomeric model, indirect evidence suggests that ORs might form dimers, which could be endowed with a distinct pharmacological profile, and, thus, be targeted to develop innovative pharmacological therapies. However, direct evidence for the spontaneous formation of OR dimers in living cells under physiological conditions is missing. Despite a growing interest in the kappa opioid receptor (KOR), KOR-selective fluorescent probes are particularly scarce in literature. Herein, we present the first set of fluorescent KOR-selective probes with antagonistic properties. Two of these were employed in single molecule microscopy (SMM) experiments to investigate KOR homodimerization, localization and trafficking. Our findings indicate that most KORs labelled with the new fluorescent probes are present as apparently freely diffusing monomers on the surface of a simple cell model.
Trans-cranial Doppler predicts early neurologic deterioration in anterior circulation ischemic stroke after successful endovascular treatment.
July 2, 2020
Helminth species specific expansion and increased TNF-alpha production of non-classical monocytes during active tuberculosis.
March 4, 2021
- ACC 2020The American College of Cardiology decided to cancel ACC.20/WCC due to COVID-19, which was scheduled to take place March 28-30 in Chicago. However, ACC.20/WCC Virtual Meeting continues to release cutting edge science and practice changing updates for cardiovascular professionals on demand and free through June 2020.
- ENDO: 2020ENDO 2020 Annual Conference has been canceled due to COVID-19. Here are highlights of emerging data that has still been released. Keep an eye out for ENDO Online 2020, which will take place from June 8 to 22.