RGS17

gene
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Also known as RGSZ2RGS-17

Summary

RGS17 (regulator of G protein signaling 17, HGNC:14088) is a protein-coding gene on chromosome 6q25.2, encoding Regulator of G-protein signaling 17 (Q9UGC6). Regulates G protein-coupled receptor signaling cascades, including signaling via muscarinic acetylcholine receptor CHRM2 and dopamine receptor DRD2.

This gene encodes a member of the regulator of G-protein signaling family. This protein contains a conserved, 120 amino acid motif called the RGS domain and a cysteine-rich region. The protein attenuates the signaling activity of G-proteins by binding to activated, GTP-bound G alpha subunits and acting as a GTPase activating protein (GAP), increasing the rate of conversion of the GTP to GDP. This hydrolysis allows the G alpha subunits to bind G beta/gamma subunit heterodimers, forming inactive G-protein heterotrimers, thereby terminating the signal.

Source: NCBI Gene 26575 — RefSeq curated summary.

At a glance

  • GWAS associations: 19
  • Clinical variants (ClinVar): 20 total
  • Druggable target: yes — 2 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_012419

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:14088
Approved symbolRGS17
Nameregulator of G protein signaling 17
Location6q25.2
Locus typegene with protein product
StatusApproved
AliasesRGSZ2, RGS-17
Ensembl geneENSG00000091844
Ensembl biotypeprotein_coding
OMIM607191
Entrez26575

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000206262, ENST00000367225, ENST00000914255

RefSeq mRNA: 1 — MANE Select: NM_012419 NM_012419

CCDS: CCDS5244

Canonical transcript exons

ENST00000206262 — 5 exons

ExonStartEnd
ENSE00001240271153131124153131282
ENSE00003890589153024262153024496
ENSE00003891788153004459153011762
ENSE00003894299153043900153044043
ENSE00003895490153026454153026543

Expression profiles

Bgee: expression breadth ubiquitous, 227 present calls, max score 86.43.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 4.7485 / max 101.8326, expressed in 1130 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter IDTPM avgSamples expressed
762754.74851130

Top tissues by expression

260 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
cortical plateUBERON:000534386.43gold quality
buccal mucosa cellCL:000233684.72gold quality
tendon of biceps brachiiUBERON:000818883.69gold quality
cartilage tissueUBERON:000241882.00gold quality
middle temporal gyrusUBERON:000277178.24gold quality
islet of LangerhansUBERON:000000677.61gold quality
ganglionic eminenceUBERON:000402376.19gold quality
Brodmann (1909) area 23UBERON:001355475.24gold quality
mucosa of paranasal sinusUBERON:000503075.14silver quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047374.54gold quality
pancreatic ductal cellCL:000207974.54silver quality
amniotic fluidUBERON:000017374.20gold quality
Brodmann (1909) area 46UBERON:000648373.72gold quality
cerebellar vermisUBERON:000472073.58gold quality
entorhinal cortexUBERON:000272872.80gold quality
ventricular zoneUBERON:000305372.69gold quality
cerebellumUBERON:000203772.54gold quality
cerebellar cortexUBERON:000212972.35gold quality
cerebellar hemisphereUBERON:000224572.22gold quality
superior frontal gyrusUBERON:000266171.93gold quality
spermCL:000001971.20silver quality
right hemisphere of cerebellumUBERON:001489071.16gold quality
postcentral gyrusUBERON:000258171.12gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099170.42gold quality
parietal lobeUBERON:000187270.07gold quality
embryoUBERON:000092270.02gold quality
primary visual cortexUBERON:000243669.90gold quality
male germ cellCL:000001569.54silver quality
prefrontal cortexUBERON:000045169.30gold quality
tendonUBERON:000004368.45gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

ExperimentMarker?Max mean expression
E-ANND-3yes5.05

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

78 targeting RGS17, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3925-3P100.0069.951237
HSA-MIR-34A-5P99.9971.211784
HSA-MIR-449A99.9971.051776
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-366299.9973.825684
HSA-MIR-32-5P99.9875.211964
HSA-MIR-92A-3P99.9875.211960
HSA-MIR-92B-3P99.9875.251955
HSA-MIR-25-3P99.9874.601817
HSA-MIR-363-3P99.9874.721821
HSA-MIR-367-3P99.9874.831819
HSA-MIR-27A-3P99.9872.132955
HSA-MIR-27B-3P99.9872.132955
HSA-MIR-998599.9872.112939
HSA-MIR-34C-5P99.9770.451577
HSA-MIR-449B-5P99.9770.261580
HSA-MIR-6888-3P99.9765.951170
HSA-MIR-495-3P99.9672.814197
HSA-MIR-568899.9673.234504
HSA-MIR-96-5P99.9572.802140
HSA-MIR-9983-3P99.9471.483631
HSA-MIR-144-3P99.9473.982698
HSA-MIR-6845-3P99.9466.881439
HSA-MIR-4760-3P99.9370.502385
HSA-MIR-1213399.9271.822006
HSA-MIR-515-5P99.9269.822343
HSA-MIR-519E-5P99.9269.622358
HSA-MIR-1271-5P99.9171.991972
HSA-MIR-3529-3P99.9073.553045
HSA-MIR-129-5P99.8870.263273

Literature-anchored findings (GeneRIF, showing 16)

  • RGS17 is a new RZ member that preferentially inhibits receptor signaling via G(i/o), G(z), and G(q) over G(s) to enhance cAMP-dependent signaling and inhibit calcium signaling (PMID:15096504)
  • RGS17, an overexpressed gene in human lung and prostate cancer, induces tumor cell proliferation through the cyclic AMP-PKA-CREB pathway. (PMID:19244110)
  • RGS17 is a major candidate for the familial lung cancer susceptibility locus on chromosome 6q23-25. (PMID:19351763)
  • Taken together, these data have provided the first evidence of miRNA regulation of RGS17 expression in lung cancer. (PMID:20420807)
  • Results establish RGS10 and RGS17 as novel regulators of cell survival and chemoresistance in ovarian cancer cells and suggest that their reduced expression may be diagnostic of chemoresistance. (PMID:21044322)
  • RGS17 is differentially expressed in hepatocellular carcinoma cells and plays a central role in regulating transformed hepatocyte tumorgenicity. (PMID:21620966)
  • Two single nucleotide polymorphisms in the regulator of G-protein signaling 17 gene are associated with smoking initiation. (PMID:22006218)
  • Variation in RGS17 was associated with risk for substance dependence diagnoses in both African American and European American populations. (PMID:22591552)
  • data suggest that RGS17 is overexpressed in colorectal carcinoma and promotes cell proliferation, migration, and invasion (PMID:28337960)
  • Taken together, the results suggested that expression of miR-203 inhibited non-small-cell lung cancer tumor growth and metastasis by targeting RGS17 (PMID:28921827)
  • A screen of over 60,000 small molecules led to the identification of five hit compounds that inhibit the RGS17-Galphao protein-protein interaction. (PMID:29351497)
  • Results showed that RGS17 overexpression promoted hepatocarcinoma (HCC) cell proliferation, migration, and invasion, and reversed the miR-199 mediated inhibition of proliferation, migration, and invasion. (PMID:29559347)
  • these findings suggest that Ca(2+) positively regulates RGS17, which may represent a general mechanism by which increased Ca(2+) concentration promotes the GAP activity of the RZ subfamily, leading to RZ-mediated inhibition of Ca(2+) signaling. (PMID:30940727)
  • Knock-down of Long non-coding RNA Linc00483 inhibited the development of cervical cancer by regulating miR-508-3p/RGS17 axis. (PMID:31454494)
  • MiR-203 inhibits cell proliferation, invasion, and migration of ovarian cancer through regulating RGS17. (PMID:34002599)
  • Hsa_circ_0000285-Mediated miR-599/RGS17 Axis Participates in the Pathogenesis of Abdominal Aortic Aneurysm by Regulating the Functions of Vascular Smooth Muscle Cells. (PMID:37094862)

Cross-species orthologs

4 orthologs

OrganismSymbolGene ID
danio_reriorgs17ENSDARG00000039435
mus_musculusRgs17ENSMUSG00000019775
rattus_norvegicusRgs17ENSRNOG00000018690
drosophila_melanogasterDhitFBGN0028743

Paralogs (23): RGS11 (ENSG00000076344), RGS1 (ENSG00000090104), AXIN1 (ENSG00000103126), RGS9 (ENSG00000108370), RGS2 (ENSG00000116741), RGS4 (ENSG00000117152), RGSL1 (ENSG00000121446), RGS13 (ENSG00000127074), RGS22 (ENSG00000132554), RGS8 (ENSG00000135824), RGS3 (ENSG00000138835), RGS5 (ENSG00000143248), RGS16 (ENSG00000143333), RGS20 (ENSG00000147509), RGS10 (ENSG00000148908), RGS18 (ENSG00000150681), RGS12 (ENSG00000159788), AXIN2 (ENSG00000168646), RGS14 (ENSG00000169220), RGS19 (ENSG00000171700), RGS6 (ENSG00000182732), RGS7 (ENSG00000182901), RGS21 (ENSG00000253148)

Protein

Protein identifiers

Regulator of G-protein signaling 17Q9UGC6 (reviewed: Q9UGC6)

All UniProt accessions (1): Q9UGC6

UniProt curated annotations — full annotation on UniProt →

Function. Regulates G protein-coupled receptor signaling cascades, including signaling via muscarinic acetylcholine receptor CHRM2 and dopamine receptor DRD2. Inhibits signal transduction by increasing the GTPase activity of G protein alpha subunits, thereby driving them into their inactive GDP-bound form. Binds selectively to GNAZ and GNAI2 subunits, accelerates their GTPase activity and regulates their signaling activities. Negatively regulates mu-opioid receptor-mediated activation of the G-proteins.

Subunit / interactions. Interacts with GNAI1 and GNAQ. Interacts with GNAZ and GNAI2. Interacts with OPRM1. Forms a complex with mu-opioid receptors and G(alpha)z/i2 subunits, including GNAZ and GNAI2; the formation of this complex results in mu-opioid receptor desensitization. Interacts with HINT1.

Subcellular location. Membrane. Synapse. Synaptosome. Nucleus. Cytoplasm.

Tissue specificity. Predominantly expressed in the cerebellum. Also expressed in the cortex and medulla. Weakly expressed in a number of peripheral tissues notably spleen, lung and leukocytes.

Post-translational modifications. N- and O-glycosylated in synapsomal membranes. Serine phosphorylated in synapsomal membranes. Sumoylated with SUMO1 and SUM02 in synaptosomes. The sumoylated forms act as a scaffold for sequestering mu-opioid receptor-activated G(alpha) subunits. Desumoylated by HINT1.

RefSeq proteins (1): NP_036551* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR016137RGSDomain
IPR036305RGS_sfHomologous_superfamily
IPR044926RGS_subdomain_2Homologous_superfamily

Pfam: PF00615

UniProt features (15 total): helix 10, chain 1, domain 1, turn 1, region of interest 1, modified residue 1

Structure

Experimental structures (PDB)

2 structures.

PDBMethodResolution (Å)
6AM3X-RAY DIFFRACTION1.53
1ZV4X-RAY DIFFRACTION2.4

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9UGC6-F179.820.64

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (1): 137

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

IDPathway
R-HSA-416476G alpha (q) signalling events
R-HSA-418594G alpha (i) signalling events
R-HSA-418597G alpha (z) signalling events

MSigDB gene sets: 150 (showing top): GSE37336_LY6C_POS_VS_NEG_NAIVE_CD4_TCELL_UP, RNGTGGGC_UNKNOWN, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, YAGI_AML_WITH_INV_16_TRANSLOCATION, GOBP_RESPONSE_TO_AMINE, REACTOME_G_ALPHA_Z_SIGNALLING_EVENTS, AAAYRNCTG_UNKNOWN, chr6q25, GOBP_RESPONSE_TO_AMPHETAMINE, DELYS_THYROID_CANCER_DN, ONDER_CDH1_TARGETS_2_UP, YAMASHITA_METHYLATED_IN_PROSTATE_CANCER, GOCC_NEURON_PROJECTION, GRYDER_PAX3FOXO1_ENHANCERS_IN_TADS, CUI_TCF21_TARGETS_2_UP

GO Biological Process (3): response to amphetamine (GO:0001975), G protein-coupled receptor signaling pathway (GO:0007186), negative regulation of signal transduction (GO:0009968)

GO Molecular Function (3): GTPase activity (GO:0003924), GTPase activator activity (GO:0005096), protein binding (GO:0005515)

GO Cellular Component (6): nucleus (GO:0005634), cytoplasm (GO:0005737), plasma membrane (GO:0005886), neuron projection (GO:0043005), synapse (GO:0045202), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-1 pathways:

CategoryPathways
GPCR downstream signalling3

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
signal transduction2
cellular anatomical structure2
response to amine1
G protein-coupled receptor activity1
regulation of signal transduction1
negative regulation of cell communication1
negative regulation of signaling1
negative regulation of response to stimulus1
ribonucleoside triphosphate phosphatase activity1
GTPase activity1
enzyme activator activity1
GTPase regulator activity1
binding1
intracellular membrane-bounded organelle1
intracellular anatomical structure1
membrane1
cell periphery1
plasma membrane bounded cell projection1
cell junction1

Protein interactions and networks

STRING

1296 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
RGS17GNB5O14775878
RGS17SUCLG2Q96I99853
RGS17GNAQP50148789
RGS17ARHGEF1Q92888788
RGS17ARHGEF11O15085785
RGS17RGSL1A5PLK6776
RGS17GRK2P25098770
RGS17RGS7BPQ6MZT1725
RGS17MCF2P10911707
RGS17GNA13Q14344707
RGS17SUCLG1P53597695
RGS17PLEKP08567689
RGS17AKAP10O43572671
RGS17PLEK2Q9NYT0668
RGS17ARHGEF25Q86VW2664

IntAct

156 interactions, top by confidence:

ABTypeScore
RGS17AQP1psi-mi:“MI:0915”(physical association)0.720
OTX1RGS17psi-mi:“MI:0915”(physical association)0.720
RGS17HOXA1psi-mi:“MI:0915”(physical association)0.720
RPL10ARGS17psi-mi:“MI:0915”(physical association)0.720
AQP1RGS17psi-mi:“MI:0915”(physical association)0.720
RGS17OTX1psi-mi:“MI:0915”(physical association)0.720
RGS17RPL10Apsi-mi:“MI:0915”(physical association)0.720
HOXA1RGS17psi-mi:“MI:0915”(physical association)0.720
NUFIP2RGS17psi-mi:“MI:0915”(physical association)0.560
RGS17GNAI3psi-mi:“MI:0915”(physical association)0.560
SMCPRGS17psi-mi:“MI:0915”(physical association)0.560
GNAI1RGS17psi-mi:“MI:0915”(physical association)0.560
PTGER3RGS17psi-mi:“MI:0915”(physical association)0.560
RGS17LCE3Cpsi-mi:“MI:0915”(physical association)0.560
RGS17LCE4Apsi-mi:“MI:0915”(physical association)0.560
RGS17LCE2Apsi-mi:“MI:0915”(physical association)0.560
RGS17psi-mi:“MI:0915”(physical association)0.560
RGS17psi-mi:“MI:0915”(physical association)0.560
RGS17NUFIP2psi-mi:“MI:0915”(physical association)0.560
RGS17GNAI1psi-mi:“MI:0915”(physical association)0.560

BioGRID (52): RGS17 (Two-hybrid), RGS17 (Two-hybrid), RGS17 (Two-hybrid), RGS17 (Two-hybrid), RGS17 (Two-hybrid), RGS17 (Two-hybrid), RGS17 (Two-hybrid), RGS17 (Two-hybrid), NUFIP2 (Two-hybrid), DHX37 (Two-hybrid), TBC1D16 (Two-hybrid), LCE4A (Two-hybrid), LCE2A (Two-hybrid), LCE3C (Two-hybrid), RGS17 (Two-hybrid)

ESM2 similar proteins: A1A643, O08849, O08850, O14921, O15539, O35119, O43665, O46470, O54829, P34295, P41220, P49758, P49800, P49802, P49803, P49806, P49808, P49809, P79100, P97844, Q08116, Q09777, Q0P5H5, Q10955, Q2KHW7, Q2M5E4, Q3S853, Q3T0T8, Q4L0E8, Q5M8L6, Q62240, Q6DGI0, Q6RG78, Q864Z2, Q8K443, Q8VYB9, Q99PG4, Q9CQE5, Q9FLY5, Q9JHX0

Diamond homologs: A1A643, F1S668, O08773, O08774, O08849, O08850, O08899, O14921, O14924, O15169, O15492, O15539, O35625, O42400, O43566, O43665, O46469, O46470, O46471, O54828, O54829, O70239, O70240, O70521, O75916, O76081, O88566, O94810, P34295, P41220, P49758, P49795, P49796, P49797, P49798, P49799, P49800, P49802, P49803, P49804

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 47 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
Formation of the cornified envelope1436.2×2e-17
Keratinization1829.5×4e-21

GO biological processes:

GO termPartnersFoldFDR
keratinization1488.6×2e-22

Disease & clinical

Clinical variants and AI predictions

ClinVar

20 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance18
Likely benign0
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1015 predictions. Top by Δscore:

VariantEffectΔscore
6:153024307:AG:Adonor_gain0.9900
6:153026447:CA:Cdonor_gain0.9900
6:153026448:ACTC:Adonor_loss0.9900
6:153026449:C:CGdonor_loss0.9900
6:153026450:TCAC:Tdonor_loss0.9900
6:153026452:A:ACdonor_gain0.9900
6:153026453:C:Adonor_loss0.9900
6:153026453:C:CCdonor_gain0.9900
6:153026453:CCATT:Cdonor_gain0.9900
6:153026478:T:Adonor_gain0.9900
6:153026539:TGAGG:Tacceptor_gain0.9900
6:153026540:GAGG:Gacceptor_gain0.9900
6:153026541:AGGCT:Aacceptor_loss0.9900
6:153026542:GG:Gacceptor_gain0.9900
6:153026542:GGCTG:Gacceptor_loss0.9900
6:153026544:C:CCacceptor_gain0.9900
6:153026544:C:Gacceptor_loss0.9900
6:153026545:T:Aacceptor_loss0.9900
6:153026549:A:ACacceptor_gain0.9900
6:153011675:T:Cdonor_gain0.9800
6:153024261:CCT:Cdonor_gain0.9800
6:153024494:TGG:Tacceptor_gain0.9800
6:153024497:C:CCacceptor_gain0.9800
6:153025863:T:TGacceptor_gain0.9800
6:153026446:ACAC:Adonor_loss0.9800
6:153026541:AGG:Aacceptor_gain0.9800
6:153026549:A:Cacceptor_gain0.9800
6:153024303:T:TAdonor_gain0.9700
6:153024492:TTTGG:Tacceptor_gain0.9700
6:153024493:TTGG:Tacceptor_gain0.9700

AlphaMissense

1401 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
6:153011637:A:CF190L1.000
6:153011637:A:TF190L1.000
6:153011638:A:GF190S1.000
6:153011639:A:GF190L1.000
6:153011640:C:AR189S1.000
6:153011640:C:GR189S1.000
6:153011641:C:AR189M1.000
6:153011641:C:GR189T1.000
6:153011642:T:AR189W1.000
6:153011642:T:CR189G1.000
6:153011650:G:AS186F1.000
6:153011652:A:CD185E1.000
6:153011652:A:TD185E1.000
6:153011653:T:AD185V1.000
6:153011653:T:CD185G1.000
6:153011653:T:GD185A1.000
6:153011654:C:AD185Y1.000
6:153011654:C:GD185H1.000
6:153011654:C:TD185N1.000
6:153011655:T:AR184S1.000
6:153011655:T:GR184S1.000
6:153011656:C:AR184I1.000
6:153011656:C:GR184T1.000
6:153011661:C:AM182I1.000
6:153011661:C:GM182I1.000
6:153011661:C:TM182I1.000
6:153011662:A:CM182R1.000
6:153011662:A:GM182T1.000
6:153011662:A:TM182K1.000
6:153011664:T:AL181F1.000

dbSNP variants (sampled 300 via entrez): RS1000005373 (6:153008883 A>G), RS1000037762 (6:153040842 T>C), RS1000050965 (6:153054650 C>T), RS1000054607 (6:153009291 C>G), RS1000064636 (6:153084328 A>G,T), RS1000069381 (6:153129791 T>A), RS1000093101 (6:153038052 A>G), RS1000112380 (6:153088852 A>G), RS1000167003 (6:153047537 C>T), RS1000260174 (6:153048654 T>C), RS1000297139 (6:153090659 C>T), RS1000298063 (6:153132423 T>C), RS1000302394 (6:153123847 T>C), RS1000311807 (6:153040934 G>C,T), RS1000352962 (6:153015949 A>G)

Disease associations

OMIM: gene MIM:607191 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

19 associations (top):

StudyTraitp-value
GCST001942_11Prostate cancer4.000000e-18
GCST003121_10Alcohol dependence5.000000e-06
GCST003127_8Lipoprotein (a) levels1.000000e-09
GCST004904_34Body mass index3.000000e-11
GCST004904_56Body mass index5.000000e-09
GCST006627_66Diastolic blood pressure1.000000e-09
GCST007325_198General risk tolerance (MTAG)2.000000e-08
GCST007565_105Morning person3.000000e-15
GCST009083_1Bacterial meningitis7.000000e-08
GCST009086_1Pneumococcal meningitis4.000000e-07
GCST009151_4High density lipoprotein cholesterol levels7.000000e-14
GCST009181_9Cuneus cortex volume7.000000e-06
GCST010241_403Apolipoprotein A1 levels1.000000e-10
GCST010242_13HDL cholesterol levels4.000000e-17
GCST010244_120Triglyceride levels1.000000e-08
GCST010988_379Adult body size4.000000e-11
GCST011320_12Type 2 diabetes or prostate cancer (pleiotropy)1.000000e-15
GCST90020025_549Waist-to-hip ratio adjusted for BMI5.000000e-09
GCST90020027_1026Waist-hip index6.000000e-09

EFO canonical traits (9, from GWAS)

EFO IDTrait name
EFO:0006925lipoprotein A measurement
EFO:0004340body mass index
EFO:0006336diastolic blood pressure
EFO:0008579risk-taking behaviour
EFO:0008328chronotype measurement
EFO:0004612high density lipoprotein cholesterol measurement
EFO:0004614apolipoprotein A 1 measurement
EFO:0004530triglyceride measurement
EFO:0007788BMI-adjusted waist-hip ratio

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4295974 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 12,011 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL417799SANGUINARIUM28,822
CHEMBL490129SANGUINARIUM CHLORIDE23,189

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

1 annotations.

VariantTypeLevelDrugsPhenotypes
rs672170Efficacy3antidepressantsMajor Depressive Disorder

PharmGKB variants

1 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs672170RGS1730.001antidepressants

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: other protein — RZ family

Most potent curated ligand interactions (8 total), top 8:

LigandActionAffinityParameter
compound I [PMID: 29351497]Inhibition5.02pIC50
celastrolInhibition4.98pIC50
compound III [PMID: 29351497]Inhibition4.84pIC50
compound V [PMID: 29351497]Inhibition4.84pIC50
compound II [PMID: 29351497]Inhibition4.72pIC50
compound IV [PMID: 29351497]Inhibition4.51pIC50
irigenolInhibition4.33pIC50
pseudochelerythrineInhibition4.14pIC50

ChEMBL bioactivities

8 potent at pChembl≥5 of 19 total, top 8 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
6.37IC50423.2nMIRIGENOL
6.15Kd714nMIRIGENOL
6.00Kd1000nMSANGUINARIUM
5.99Kd1020nMSANGUINARIUM CHLORIDE
5.86IC501386nMSANGUINARIUM CHLORIDE
5.22IC506000nMCELASTROL
5.20IC506359nMCELASTROL
5.00IC501e+04nMGAMBOGIC ACID

PubChem BioAssay actives

3 with measured affinity, of 30 total; 3 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
24-methyl-5,7,18,20-tetraoxa-24-azoniahexacyclo[11.11.0.02,10.04,8.014,22.017,21]tetracosa-1(24),2,4(8),9,11,13,15,17(21),22-nonaene1377216: Binding affinity to RGS17 (unknown origin) by ITC methodkd1.0000uM
(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid1377215: Inhibition of RGS17 (unknown origin) GAP activity in presence of GTP by malachite green dye based assayic506.0000uM
(Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoic acid1377215: Inhibition of RGS17 (unknown origin) GAP activity in presence of GTP by malachite green dye based assayic5010.0000uM

CTD chemical–gene interactions

43 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Valproic Acidaffects expression, increases expression, increases methylation3
Particulate Matterincreases abundance, affects cotreatment, increases expression, decreases expression3
Benzo(a)pyreneaffects methylation, increases methylation2
Cisplatinincreases response to substance, affects cotreatment, decreases expression2
Phenylmercuric Acetateaffects cotreatment, decreases expression2
aristolochic acid Idecreases expression1
GSK-J4decreases expression1
triphenyl phosphateaffects expression1
terbufosincreases methylation1
trichostatin Aincreases expression, decreases expression1
tris(1,3-dichloro-2-propyl)phosphateincreases expression1
aflatoxin B2affects methylation1
hydroquinoneincreases expression1
isobutyl alcoholaffects cotreatment, decreases expression, increases abundance1
di-n-butylphosphoric acidaffects expression1
2-palmitoylglycerolincreases expression1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamideaffects cotreatment, decreases expression1
2,2’,4,4’,5-brominated diphenyl etherincreases expression1
abrineincreases expression1
dorsomorphinaffects cotreatment, decreases expression1
jinfukangaffects cotreatment, decreases expression1
Docetaxelincreases response to substance1
Resveratrolaffects cotreatment, decreases expression1
Temozolomidedecreases expression1
Fulvestrantdecreases methylation1
Air Pollutantsdecreases expression, increases abundance1
Arsenicaffects methylation1
Vehicle Emissionsincreases methylation1
Calcitriolincreases expression, affects cotreatment1
Diazinondecreases methylation1

ChEMBL screening assays

20 unique, capped per target: 20 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL4191647BindingInhibition of RGS17 (unknown origin) GAP activity in presence of GTP by malachite green dye based assayNatural Products Discovered in a High-Throughput Screen Identified as Inhibitors of RGS17 and as Cytostatic and Cytotoxic Agents for Lung and Prostate Cancer Cell Lines. — J Nat Prod

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.