Molecular mechanism of biased signaling at the kappa opioid receptor [PDF]
Nature Communications, 2023 Biased signaling in κ-opiod receptors (KOR) offer an attractive strategy for pain management. Here the authors identify determinants of KOR signaling bias using structural methods in combination with molecular dynamics simulations.
Amal El Daibani +13 more
doaj +3 more sources
The Kappa Opioid Receptor: A Promising Therapeutic Target for Multiple Pathologies [PDF]
Frontiers in Pharmacology, 2022 Kappa-opioid receptors (KOR) are widely expressed throughout the central nervous system, where they modulate a range of physiological processes depending on their location, including stress, mood, reward, pain, inflammation, and remyelination.
Martin L. Dalefield +3 more
doaj +3 more sources
In Vitro, In Vivo and In Silico Characterization of a Novel Kappa-Opioid Receptor Antagonist [PDF]
Pharmaceuticals, 2022 Kappa-opioid receptor (KOR) antagonists are promising innovative therapeutics for the treatment of the central nervous system (CNS) disorders. The new scaffold opioid ligand, Compound A, was originally found as a mu-opioid receptor (MOR) antagonist but ...
Kristina Puls +6 more
doaj +4 more sources
Design and structural validation of peptide-drug conjugate ligands of the kappa-opioid receptor. [PDF]
Nat Commun, 2023 Despite the increasing number of GPCR structures and recent advances in peptide design, the development of efficient technologies allowing rational design of high-affinity peptide ligands for single GPCRs remains an unmet challenge.
Muratspahić E +23 more
europepmc +2 more sources
Nanobody-enabled monitoring of kappa opioid receptor states
Nature Communications, 2020 Recent studies revealed that G protein-coupled receptors rapidly interconvert between multiple states. Here, authors use the kappa opioid receptor (KOR) and show how two state-dependent nanobodies provide real-time reporting of ligand stabilized states ...
Tao Che +13 more
doaj +2 more sources
In vitro and in vivo Pharmacological Activities of 14-O-Phenylpropyloxymorphone, a Potent Mixed Mu/Delta/Kappa-Opioid Receptor Agonist With Reduced Constipation in Mice [PDF]
Frontiers in Pharmacology, 2018 Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Roberta Lattanzi +4 more
doaj +4 more sources
Major Depressive Disorder and Kappa Opioid Receptor [PDF]
Translational Perioperative and Pain Medicine, 2016 Major depressive disorder (MDD) is a common psychiatric disease worldwide. The clinical use of tricyclic antidepressants (TCAs), monoamine oxidase inhibitors (MAOIs) and selective serotonin reuptake inhibitors (SSRIs)/serotonin–norepinephrine reuptake ...
Wei Li +7 more
openalex +2 more sources
Signaling underlying kappa opioid receptor-mediated behaviors in rodents [PDF]
Frontiers in Neuroscience, 2022 Kappa opioid receptor (KOR) agonists are potentially useful as analgesic and anti-pruritic agents, for prevention and treatment of substance use disorders, and for treatment of demyelinating diseases.
Lee-Yuan Liu-Chen, Peng Huang
doaj +2 more sources
Synthesis, Biological Evaluation, and SAR Studies of 14β-phenylacetyl Substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones Derivatives: Ligands With Mixed NOP and Opioid Receptor Profile [PDF]
Frontiers in Psychiatry, 2018 A series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and delta (DOP) opioid receptors and nociceptin/orphanin FQ peptide (NOP ...
Vinod Kumar +6 more
doaj +6 more sources
International Journal of Neuropsychopharmacology, 2018 Background The kappa opioid receptor system has been revealed as a potential pharmacotherapeutic target for the treatment of addictions to substances of abuse.
Amelia Dunn +5 more
openalex +2 more sources