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

SIGMAR1 (Q99720) - Overview - Molecular Target Synopsis

Protein


SIGMAR1, Sigma non-opioid intracellular receptor 1
UniProt Q99720

Also Known as SGMR1_HUMAN, SIGMAR1, OPRS1, SRBP

Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma membrane. Involved in the regulation of different receptors it plays a role in BDNF signaling and EGF signaling. Also regulates ion channels like the potassium channel and could modulate neurotransmitter release. Plays a role in calcium signaling through modulation together with ANK2 of the ITP3R-dependent calcium efflux at the endoplasmic reticulum. Plays a role in several other cell functions including proliferation, survival and death. Originally identified for its ability to bind various psychoactive drugs it is involved in learning processes, memory and mood alteration (PubMed:16472803, PubMed:9341151). Necessary for proper mitochondrial axonal transport in motor neurons, in particular the retrograde movement of mitochondria. Homotrimer (PubMed:27042935). Forms a ternary complex with ANK2 and ITPR3. The complex is disrupted by agonists. Interacts with KCNA4 (By similarity). Interacts with KCNA2; cocaine consumption leads to increased interaction.

5HK1 deposition date (2016-01-13)
HUMAN SIGMA-1 RECEPTOR BOUND TO PD144418
RCSB/PDB
Inspect Structure
See all 3D Structures for SIGMAR1

Isoforms / Transcripts (Protein Coding)


Drugs


SIGMAR1 is targeted by Approved Drugs Acetophenazine, Dextromethorphan. (see details)
Acetophenazine
Dextromethorphan

Sub-cellular localization


UniProt: SIGMAR1 is active in the following subcellular-locations: cell junction, cell membrane, cell projection, cytoplasmic vesicle, endoplasmic reticulum membrane, growth cone, lipid droplet, membrane, nucleus envelope, nucleus inner membrane, nucleus outer membrane, postsynaptic cell membrane, postsynaptic density, synapse.
GO terms: SIGMAR1 is active in the following subcellular-locations: cell junction, cytoplasmic vesicle, endoplasmic reticulum, endoplasmic reticulum membrane, growth cone, integral component of membrane, integral component of plasma membrane, lipid droplet, nuclear envelope, nuclear inner membrane, nuclear outer membrane, postsynaptic density, postsynaptic membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project SIGMAR1 has gain in 6 cell-lines, loss in 3 cell-lines and no signal in 996 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: RPMI_8226, BT_549, UACC_62

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SCC-9, BFTC-905, LS1034

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: HeLa-S3, HMEC, A549

(see details)

RNA Interference


SIGMAR1 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)

3D Structures


There are 2 structures (6 chains) solved for SIGMAR1
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


SIGMAR1 has been screened with 3112 compounds (5042 bioactivities), 1762 compounds have bioactivities that show binding affinity of <= 500nM (2266 bioactivities). (see details)