Structure-based design of bitopic ligands for the µ-opioid receptor
Mu-opioid receptor (µOR) agonists such as fentanyl have long been used for pain
management, but are considered a major public health concern owing to their adverse side …
management, but are considered a major public health concern owing to their adverse side …
AG protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine
SM DeWire, DS Yamashita, DH Rominger, G Liu… - … of Pharmacology and …, 2013 - ASPET
The concept of ligand bias at G protein-coupled receptors broadens the possibilities for
agonist activities and provides the opportunity to develop safer, more selective therapeutics …
agonist activities and provides the opportunity to develop safer, more selective therapeutics …
Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro …
XT Chen, P Pitis, G Liu, C Yuan… - Journal of medicinal …, 2013 - ACS Publications
The concept of “ligand bias” at G protein coupled receptors has been introduced to describe
ligands which preferentially stimulate one intracellular signaling pathway over another …
ligands which preferentially stimulate one intracellular signaling pathway over another …
Crystal structure of the µ-opioid receptor bound to a morphinan antagonist
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 …
among the most used clinical drugs to relieve severe pain. These prototypical opioids …
[HTML][HTML] Critical assessment of G protein-biased agonism at the μ-opioid receptor
A Gillis, A Kliewer, E Kelly, G Henderson… - Trends in …, 2020 - cell.com
G protein-biased agonists of the μ-opioid receptor (MOPr) have been proposed as an
improved class of opioid analgesics. Recent studies have been unable to reproduce the …
improved class of opioid analgesics. Recent studies have been unable to reproduce the …
[HTML][HTML] How μ-opioid receptor recognizes fentanyl
Roughly half of the drug overdose-related deaths in the United States are related to
synthetic opioids represented by fentanyl which is a potent agonist of mu-opioid receptor …
synthetic opioids represented by fentanyl which is a potent agonist of mu-opioid receptor …
Molecular recognition of morphine and fentanyl by the human μ-opioid receptor
Morphine and fentanyl are among the most used opioid drugs that confer analgesia and
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …
Structural insights into µ-opioid receptor activation
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …
Identification of a μ-δ opioid receptor heteromer-biased agonist with antinociceptive activity
I Gomes, W Fujita, A Gupta… - Proceedings of the …, 2013 - National Acad Sciences
G protein-coupled receptors play a pivotal role in many physiological signaling pathways.
Mounting evidence suggests that G protein-coupled receptors, including opioid receptors …
Mounting evidence suggests that G protein-coupled receptors, including opioid receptors …
Structure-based discovery of opioid analgesics with reduced side effects
Morphine is an alkaloid from the opium poppy used to treat pain. The potentially lethal side
effects of morphine and related opioids—which include fatal respiratory depression—are …
effects of morphine and related opioids—which include fatal respiratory depression—are …
相关搜索
- µ opioid bitopic ligands
- μ opioid receptor agonists
- µ opioid receptor activation
- µ opioid crystal structure
- µ opioid morphinan antagonist
- μ opioid morphine and fentanyl
- opioid receptor antinociceptive activity
- μ opioid molecular recognition
- μ opioid critical assessment
- opioid receptor μ δ
- µ opioid structural insights