Page last updated: 2024-10-24

kappa-type opioid receptor binding

Definition

Target type: molecularfunction

Binding to a kappa-type opioid receptor. [GOC:mah, GOC:nln]

Kappa-type opioid receptors (KORs) are G protein-coupled receptors that mediate the physiological effects of the endogenous opioid peptides dynorphin and endomorphin, as well as exogenous opioid drugs such as the synthetic opioid ketocyclazocine. Upon ligand binding, KORs activate a signaling cascade involving the heterotrimeric G protein Gi/o, which in turn inhibits adenylate cyclase activity, leading to a decrease in intracellular cAMP levels. This pathway can lead to a variety of cellular responses, including modulation of neuronal excitability, pain perception, and reward pathways. KORs are also implicated in the regulation of stress responses, anxiety, and addiction. The molecular function of KOR binding involves a complex interplay of receptor structure, ligand binding, and downstream signaling events. The receptor's seven transmembrane domains are responsible for the binding of opioid ligands. Upon ligand binding, the receptor undergoes a conformational change that activates its intracellular signaling domains. This activation triggers the interaction with Gi/o proteins, leading to the inhibition of adenylate cyclase and the activation of other intracellular signaling pathways. The specific molecular events involved in KOR activation and signaling are still under investigation, but it is clear that the binding of ligands to the receptor is a crucial step in the process.'
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Proteins (1)

ProteinDefinitionTaxonomy
Interleukin-2An interleukin-2 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P60568]Homo sapiens (human)

Compounds (7)

CompoundDefinitionClassesRoles
daidzindaidzein 7-O-beta-D-glucoside : A glycosyloxyisoflavone that is daidzein attached to a beta-D-glucopyranosyl residue at position 7 via a glycosidic linkage. It is used in the treatment of alcohol dependency (antidipsotropic).

daidzin: a potent, selective, and reversible inhibitor of human mitochondrial aldehyde dehydrogenase
7-hydroxyisoflavones 7-O-beta-D-glucoside;
hydroxyisoflavone;
monosaccharide derivative
plant metabolite
ononin4'-methoxyisoflavones;
7-hydroxyisoflavones 7-O-beta-D-glucoside;
monosaccharide derivative
plant metabolite
formononetin4'-methoxyisoflavones;
7-hydroxyisoflavones
phytoestrogen;
plant metabolite
luteolin-7-glucosideluteolin 7-O-beta-D-glucoside : A glycosyloxyflavone that is luteolin substituted by a beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage.

luteolin-7-glucoside: has both antiasthmatic and antineoplastic activities; has 3C protease inhibitory activity; isolated from Ligustrum lucidum
beta-D-glucoside;
glycosyloxyflavone;
monosaccharide derivative;
trihydroxyflavone
antioxidant;
plant metabolite
N(2)-carbamimidoyl-N-{2-[4-(3-{4-[(5-carboxyfuran-2-yl)methoxy]-2,3-dichlorophenyl}-1-methyl-1H-pyrazol-5-yl)piperidin-1-yl]-2-oxoethyl}-D-leucinamideN(2)-carbamimidoyl-N-{2-[4-(3-{4-[(5-carboxyfuran-2-yl)methoxy]-2,3-dichlorophenyl}-1-methyl-1H-pyrazol-5-yl)piperidin-1-yl]-2-oxoethyl}-D-leucinamide : A leucine derivative obtained by fpormal condensation of the secondary amino group of 5-({2,3-dichloro-4-[1-methyl-5-(piperidin-4-yl)-1H-pyrazol-3-yl]phenoxy}methyl)-2-furoic acid and the carboxy group of N-amidino-L-leucylglycineD-leucine derivative;
dichlorobenzene;
furoic acid;
glycine derivative;
guanidines;
pyrazolylpiperidine
calycosin-7-o-beta-d-glucopyranosidecalycosin-7-O-beta-D-glucoside : A glycosyloxyisoflavone that is calycosin substituted by a beta-D-glucopyranosyl residue at position at 7 via a glycosidic linkage.

calycosin-7-O-beta-D-glucoside: from Radix Astragali
4'-methoxyisoflavones;
7-hydroxyisoflavones 7-O-beta-D-glucoside;
hydroxyisoflavone;
monosaccharide derivative
diosgenin glucosidediosgenin 3-O-beta-D-glucoside : A sterol 3-beta-D-glucoside having diosgenin as the sterol component.

diosgenin glucoside: RN given refers to (3beta,25R)-isomer; structure given in first source
hexacyclic triterpenoid;
monosaccharide derivative;
spiroketal;
sterol 3-beta-D-glucoside
metabolite