Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities
X Jiang, K Wu, R Bai, P Zhang, Y Zhang - European Journal of Medicinal …, 2022 - Elsevier
Quinoxalinones are a class of heterocyclic compounds which attract extensive attention
owing to their potential in the field of organic synthesis and medicinal chemistry. During the …
owing to their potential in the field of organic synthesis and medicinal chemistry. During the …
A review of the therapeutic potential of recently developed G protein-biased kappa agonists
KL Mores, BR Cummins, RJ Cassell… - Frontiers in …, 2019 - frontiersin.org
Between 2000 and 2005 several studies revealed that morphine is more potent and exhibits
fewer side effects in beta-arrestin 2 knockout mice. These findings spurred efforts to develop …
fewer side effects in beta-arrestin 2 knockout mice. These findings spurred efforts to develop …
Biased ligands of G protein-coupled receptors (GPCRs): Structure–functional selectivity relationships (SFSRs) and therapeutic potential
L Tan, W Yan, JD McCorvy, J Cheng - Journal of medicinal …, 2018 - ACS Publications
G protein-coupled receptors (GPCRs) signal through both G-protein-dependent and G-
protein-independent pathways, and β-arrestin recruitment is the most recognized one of the …
protein-independent pathways, and β-arrestin recruitment is the most recognized one of the …
Design and structural validation of peptide–drug conjugate ligands of the kappa-opioid receptor
E Muratspahić, K Deibler, J Han, N Tomašević… - Nature …, 2023 - nature.com
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 …
the development of efficient technologies allowing rational design of high-affinity peptide …
[HTML][HTML] The kappa opioid receptor: a promising therapeutic target for multiple pathologies
ML Dalefield, B Scouller, R Bibi… - Frontiers in Pharmacology, 2022 - frontiersin.org
Kappa-opioid receptors (KOR) are widely expressed throughout the central nervous system,
where they modulate a range of physiological processes depending on their location …
where they modulate a range of physiological processes depending on their location …
TLR4 biased small molecule modulators
Biased pharmacological modulators provide potential therapeutic benefits, including greater
pharmacodynamic specificity, increased efficiency and reduced adverse effects. Therefore …
pharmacodynamic specificity, increased efficiency and reduced adverse effects. Therefore …
Development of functionally selective, small molecule agonists at kappa opioid receptors
L Zhou, KM Lovell, KJ Frankowski, SR Slauson… - Journal of Biological …, 2013 - ASBMB
The kappa opioid receptor (KOR) is widely expressed in the CNS and can serve as a means
to modulate pain perception, stress responses, and affective reward states. Therefore, the …
to modulate pain perception, stress responses, and affective reward states. Therefore, the …
Emerging structural insights into biased GPCR signaling
The discovery of biased signaling at G protein-coupled receptors (GPCRs), the largest class
of cell surface receptors and primary drug targets for numerous human diseases, has …
of cell surface receptors and primary drug targets for numerous human diseases, has …
A systematic review on the kappa opioid receptor and its ligands: New directions for the treatment of pain, anxiety, depression, and drug abuse
Kappa opioid receptor (KOR) is a member of the opioid receptor system, the G protein-
coupled receptors that are expressed throughout the peripheral and central nervous …
coupled receptors that are expressed throughout the peripheral and central nervous …
Strategies for developing κ opioid receptor agonists for the treatment of pain with fewer side effects
KF Paton, DV Atigari, S Kaska, T Prisinzano… - Journal of Pharmacology …, 2020 - ASPET
There is significant need to find effective, nonaddictive pain medications. κ Opioid receptor
(KOPr) agonists have been studied for decades but have recently received increased …
(KOPr) agonists have been studied for decades but have recently received increased …