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Tclin
HMGCR
3-hydroxy-3-methylglutaryl-coenzyme A reductase

Protein Summary
Description
Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins. HMG-CoA reductase is the rate-limiting enzyme for cholesterol synthesis and is regulated via a negative feedback mechanism mediated by sterols and non-sterol metabolites derived from mevalonate, the product of the reaction catalyzed by reductase. Normally in mammalian cells this enzyme is suppressed by cholesterol derived from the internalization and degradation of low density lipoprotein (LDL) via the LDL receptor. Competitive inhibitors of the reductase induce the expression of LDL receptors in the liver, which in turn increases the catabolism of plasma LDL and lowers the plasma concentration of cholesterol, an important determinant of atherosclerosis. Alternatively spliced transcript variants encoding different isoforms have been found for this gene ...more
Uniprot Accession IDs
Gene Name
Ensembl ID
  • ENST00000287936
  • ENSP00000287936
  • ENSG00000113161
  • ENST00000343975
  • ENSP00000340816
  • ENST00000511206
  • ENSP00000426745

Symbol
  • LDLCQ3
Illumination Graph
Knowledge Table
Most Knowledge About
Knowledge Value (0 to 1 scale)
biological process
1
ligand (chemical)
1
protein domain
0.99
chemical
0.93
transcription factor binding site profile
0.92


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: 1926.93   (req: < 5)
Gene RIFs: 102   (req: <= 3)
Antibodies: 310   (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: 1926.93   (req: >= 5)
Gene RIFs: 102   (req: > 3)
Antibodies: 310   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 29
Tchem

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

Active Ligands: 218
Tclin

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

Active Drugs: 9
Protein Sequence and Structure
Residue Counts
Protein Sequence
ProtVista Viewer
Related Tools
Target Illumination GWAS Analytics (TIGA)
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TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.
GENEVA
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GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.
GlyGen
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GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.
ARCHS4
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ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.
Approved Drugs (9)
1 – 9 of 9
atorvastatin
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bezafibrate
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cerivastatin
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lovastatin
Rendered image for lovastatin
pitavastatin
Rendered image for pitavastatin
pravastatin
Rendered image for pravastatin
rosuvastatin
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simvastatin
Rendered image for simvastatin
fluvastatin
Rendered image for fluvastatin
Active Ligands (218)
1 – 10 of 218
25-hydroxycholesterol
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US9353061, Lova-HA (1)
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CHEMBL2347007
Rendered image for CHEMBL2347007
CHEMBL2347006
Rendered image for CHEMBL2347006
CHEMBL2347008
Rendered image for CHEMBL2347008
CHEMBL2347005
Rendered image for CHEMBL2347005
CHEMBL2347009
Rendered image for CHEMBL2347009
CHEMBL2347011
Rendered image for CHEMBL2347011
US9115116, 6b
Rendered image for US9115116, 6b
CHEMBL2347010
Rendered image for CHEMBL2347010
Protein-Protein Interactions (243)
1 – 10 of 243
PTCHD3
Tbio
Novelty:  0.00081643
p_int:  0.992128034
p_ni:  0.007871966
Data Source:  BioPlex
GABRA6
Tclin
Family:  IC
Novelty:  0.02894664
p_int:  0.97357521
p_ni:  0.026424789
Score:  0.187
Data Source:  BioPlex,STRINGDB
ADGRG5
Tdark
Family:  GPCR
Novelty:  0.26575982
p_int:  0.942366167
p_ni:  0.057633833
Data Source:  BioPlex
CCR6
Tchem
Family:  GPCR
Novelty:  0.00257933
p_int:  0.931968933
p_ni:  0.068031067
Data Source:  BioPlex
PTGIR
Tclin
Family:  GPCR
Novelty:  0.0091906
p_int:  0.91768648
p_ni:  0.08231352
Score:  0.159
Data Source:  BioPlex,STRINGDB
CD209
Tchem
Novelty:  0.001172
p_int:  0.91367529
p_ni:  0.08632471
Score:  0.345
Data Source:  BioPlex,STRINGDB
ACVR1C
Tbio
Family:  Kinase
Novelty:  0.01675672
p_int:  0.907917318
p_ni:  0.092082682
Data Source:  BioPlex
KCNS3
Tclin
Family:  IC
Novelty:  0.05882087
p_int:  0.893074814
p_ni:  0.106925125
p_wrong:  6.1e-8
Score:  0.185
Data Source:  BioPlex,STRINGDB
ADCY9
Tbio
Family:  Enzyme
Novelty:  0.00744116
p_int:  0.84682935
p_ni:  0.15317065
Data Source:  BioPlex
OR13J1
Tdark
Family:  oGPCR
Novelty:  2.15311005
p_int:  0.765481356
p_ni:  0.234518636
p_wrong:  7e-9
Data Source:  BioPlex
Pathways (57)
Activation of gene expression by SREBF (SREBP) (R-HSA-2426168)

Click on a row in the table to change the structure displayed.

Items per page:
1 – 5 of 8
Data Source
Name
Explore in Pharos
Explore in Source
Reactome
Activation of gene expression by SREBF (SREBP)
Reactome
Cholesterol biosynthesis
Reactome
Metabolism
Reactome
Metabolism of lipids
Reactome
Metabolism of steroids
Name
Explore in Pharos
Explore in Source
Activation of gene expression by SREBF (SREBP)
Cholesterol biosynthesis
Metabolism
Metabolism of lipids
Metabolism of steroids
Gene Ontology Terms (33)
Items per page:
10
1 – 6 of 6
GO Term
Evidence
Assigned by
Inferred from Direct Assay (IDA)
UniProtKB
Inferred from Direct Assay (IDA)
UniProtKB
Inferred from Direct Assay (IDA)
UniProtKB
Inferred from Biological aspect of Ancestor (IBA)
GO_Central
Inferred from Electronic Annotation (IEA)
Ensembl
Inferred from Electronic Annotation (IEA)
Ensembl
GWAS Traits (15)
GWAS Trait
EFO ID
Study Count
SNP Count
Beta Count
Odds Ratio
Evidence (Mean Rank Score)
Provenance
low density lipoprotein cholesterol measurement
19
18
34
2.8
99.9
total cholesterol measurement
12
15
24
3.2
99.4
apolipoprotein B measurement
2
5
5
98.6
HMG CoA reductase inhibitor use measurement
1
1
1
76.5
platelet count
1
1
1
71.9
GWAS Trait
EFO ID
Beta Count
Odds Ratio
Evidence (Mean Rank Score)
Provenance
low density lipoprotein cholesterol measurement
34
2.8
99.9
total cholesterol measurement
24
3.2
99.4
apolipoprotein B measurement
5
98.6
HMG CoA reductase inhibitor use measurement
1
76.5
platelet count
1
71.9
Find similar targets by:
Orthologs (17)
1 – 5 of 17
Species
Name
Source ID
Gene ID
OMA
EggNOG
Inparanoid
Chimp
3-hydroxy-3-methylglutaryl-CoA reductase
VGNC:4034
471516
Macaque
3-hydroxy-3-methylglutaryl-CoA reductase
705479
Mouse
MGI:96159
15357
Rat
RGD:2803
25675
Dog
3-hydroxy-3-methylglutaryl-CoA reductase
VGNC:41714
479182
Species
Name
OMA
EggNOG
Inparanoid
Chimp
3-hydroxy-3-methylglutaryl-CoA reductase
Macaque
3-hydroxy-3-methylglutaryl-CoA reductase
Mouse
Rat
Dog
3-hydroxy-3-methylglutaryl-CoA reductase
Publication Statistics
PubMed Score 1926.93
PubMed score by year
PubTator Score 2539.38
PubTator score by year