Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

Oprk1 (P34975) - Overview - Molecular Target Synopsis

Protein


Oprk1, Kappa-type opioid receptor
UniProt P34975

Also Known as OPRK_RAT, Oprk1, Ror-d

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. Interacts with SLC9A3R1. Interacts with GABARAPL1.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
380P34975-1

Sub-cellular localization


UniProt: Oprk1 is active in the following subcellular-locations: cell membrane.
GO terms: Oprk1 is active in the following subcellular-locations: axon terminus, cytosol, dendrite, integral component of membrane, integral component of plasma membrane, neuronal cell body, nucleus, perikaryon, plasma membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project Oprk1 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

RNA Interference


Oprk1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: . (see details)


Screening and Chemistry


Oprk1 has been screened with 1001 compounds (1725 bioactivities), 475 compounds have bioactivities that show binding affinity of <= 500nM (733 bioactivities). (see details)