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. [provided by RefSeq, Aug 2008]

Uniprot Accession IDs

• P04035
• B7Z3Y9
• Q8N190
• HMG-CoA reductase

Gene Name

• HMGCR

Ensembl ID

• ENST00000287936
• ENSP00000287936
• ENSG00000113161
• ENST00000343975
• ENSP00000340816
• ENST00000511206
• ENSP00000426745

Symbol

• LDLCQ3

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

Protein Classes

No PANTHER Classes or DTO Classes found

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: 4011.83   (req: < 5)

Gene RIFs: 131   (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: 4011.83   (req: >= 5)

Gene RIFs: 131   (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: 223

Tclin

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

Active Drugs: 9