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المؤلفPineyro, Graciela
المؤلفNagi, Karim
تاريخ الإتاحة2021-01-24T11:10:35Z
تاريخ النشر2020-12-27
اسم المنشورCellular Signalling
المعرّفhttp://dx.doi.org/10.1016/j.cellsig.2020.109906
الاقتباسGraciela Pineyro, Karim Nagi, Signaling diversity of mu- and delta- opioid receptor ligands: Re-evaluating the benefits of β-arrestin/G protein signaling bias, Cellular Signalling, Volume 80, 2021, 109906
الرقم المعياري الدولي للكتاب0898-6568
معرّف المصادر الموحدhttp://hdl.handle.net/10576/17364
الملخصOpioid analgesics are elective for treating moderate to severe pain but their use is restricted by severe side effects. Signaling bias has been proposed as a viable means for improving this situation. To exploit this opportunity, continuous efforts are devoted to understand how ligand-specific modulations of receptor functions could mediate the different in vivo effects of opioids. Advances in the field have led to the development of biased agonists based on hypotheses that allocated desired and undesired effects to specific signaling pathways. However, the prevalent hypothesis associating β-arrestin to opioid side effects was recently challenged and multiple of the newly developed biased drugs may not display the superior side effects profile that was sought. Moreover, biased agonism at opioid receptors is now known to be time- and cell-dependent, which adds a new layer of complexity for bias estimation. Here, we first review the signaling mechanisms underlying desired and undesired effects of opioids. We then describe biased agonism at opioid receptors and discuss the different perspectives that support the desired and undesired effects of opioids in view of exploiting biased signaling for therapeutic purposes. Finally, we explore how signaling kinetics and cellular background can influence the magnitude and directionality of bias at those receptors.
اللغةen
الناشرElsevier
الموضوعArrestin
Bias
Biased agonism
Functional selectivity
Kinetics
Opioid
العنوانSignaling diversity of mu- and delta- opioid receptor ligands: Re-evaluating the benefits of β-arrestin/G protein signaling bias.
النوعArticle
رقم المجلد80
dc.accessType Open Access


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