Tclin OPRK1 Kappa-type opioid receptor

Protein Summary

Description

G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions. This gene encodes an opioid receptor, which is a member of the 7 transmembrane-spanning G protein-coupled receptor family. It functions as a receptor for endogenous ligands, as well as a receptor for various synthetic opioids. Ligand binding results in inhibition of adenylate cyclase activity and neurotransmitter release. This opioid receptor plays a role in the perception of pain and mediating the hypolocomotor, analgesic and aversive actions of synthetic opioids. Variations in this gene have also been associated with alcohol dependence and opiate addiction. Alternatively spliced transcript variants encoding different isoforms have been found for this gene. A recent study provided evidence for translational readthrough in this gene, and expression of an additional C-terminally extended isoform via the use of an alternative in-frame translation termination codon. [provided by RefSeq, Dec 2017]

Uniprot Accession IDs

• P41145
• E5RHC9
• Q499G4
• K-OR-1

Gene Name

• OPRK1

Ensembl ID

• ENST00000265572
• ENSP00000265572
• ENSG00000082556
• ENST00000520287
• ENSP00000429706
• ENST00000524278
• ENSP00000430923
• ENST00000612786
• ENSP00000483000

Symbol

• OPRK
• KOR
• OPRK
• KOR-1
• K-OR-1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
ligand (chemical)	1
drug	0.99
chemical	0.78
PubMedID	0.7
biological term	0.69

Protein Classes

PANTHER Classes

Protein / Receptor / G-protein Coupled Receptor / Kappa-type Opioid Receptor

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Kappa-type Opioid Receptor

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 794.9   (req: < 5)

Gene RIFs: 97   (req: <= 3)

Antibodies: 370   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 794.9   (req: >= 5)

Gene RIFs: 97   (req: > 3)

Antibodies: 370   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 39

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 2285

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 17