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HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase) is an enzyme. The public catalogues list it as a drug target, and clinical evidence ties its variants to diagnosis, prognosis or drug response.
Catalyses the conversion of (3S)-hydroxy-3-methylglutaryl-CoA (HMG-CoA) to mevalonic acid, the rate-limiting step in the synthesis of cholesterol and other isoprenoids, thus plays a critical role in cellular cholesterol homeostasis. HMGCR is the main target of statins, a class of cholesterol-lowering drugs.
Open Targets scores its association with cancer at 0.51 (direct and indirect evidence; datatypes literature 0.98, animal model 0.39, genetic association 0.39, clinical 0.68).
In plain words · HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase) is an enzyme. The public catalogues list it as a drug target, and clinical evidence ties its variants to diagnosis, prognosis or drug response.
HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase) is an enzyme. The public catalogues list it as a drug target, and clinical evidence ties its variants to diagnosis, prognosis or drug response.
Catalyses the conversion of (3S)-hydroxy-3-methylglutaryl-CoA (HMG-CoA) to mevalonic acid, the rate-limiting step in the synthesis of cholesterol and other isoprenoids, thus plays a critical role in cellular cholesterol homeostasis.
No product in this corpus aims at HMGCR yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
Broadly expressed or essential: HPA lists HMGCR among essential proteins; a medicine acting on the wild-type protein would expose normal tissue too. HPA HMGCR: RNA tissue enhanced (liver 99 nTPM); high antibody staining in 11 normal tissues; highest cancer staining colorectal cancer (8 of 11 high). Distribution: no corpus cancer carries a prevalence row, threshold or catalogue link for it; Open Targets associates it with 0 specific cancer types at or above 0.5. (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas HMGCR tissue; Open Targets ENSG00000113161 associations
First described 1985. Earliest sequence paper UniProt cites for the protein: Luskey K.L. et al, J. Biol. Chem, 1985, "Human 3-hydroxy-3-methylglutaryl coenzyme A reductase. Conserved domains responsible for catalytic activity and sterol-regulated degradation". Source.
Sources: HGNC HGNC:5006 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P04035 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000113161 (association with cancer (MONDO_0004992) 0.51; (GraphQL API, CC0))
Catalyses the conversion of (3S)-hydroxy-3-methylglutaryl-CoA (HMG-CoA) to mevalonic acid, the rate-limiting step in the synthesis of cholesterol and other isoprenoids, thus plays a critical role in cellular cholesterol homeostasis. HMGCR is the main target of statins, a class of cholesterol-lowering drugs. Location: Endoplasmic reticulum membrane; Peroxisome membrane (UniProt). Locus 5q13.3 (HGNC).
RNA: tissue enhanced (liver 99 nTPM), detected in all normal tissues.
Medium: Adrenal gland, Bone marrow, Breast, Bronchus, Caudate, Cerebellum, Cervix, Colon.
Medium only: breast cancer, carcinoid, endometrial cancer, glioma.
HPA HMGCR tissue · HPA HMGCR pathology · HPA protein class: Essential proteins, FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
Query for this target: (TITLE:"HMGCR" OR ABSTRACT:"HMGCR" OR TITLE:"3-hydroxy-3-methylglutaryl-CoA reductase" OR ABSTRACT:"3-hydroxy-3-methylglutaryl-CoA reductase" OR TITLE:"3-hydroxy-3-methylglutaryl-coenzyme A reductase" OR ABSTRACT:"3-hydroxy-3-methylglutaryl-coenzyme A reductase") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about HMGCR, not a curated reading list.