HMGCR
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.
Overview
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).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
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.
- 3 · How drugs use it
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.
External identifiers
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))
Biology
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).
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: Open Targets known-drug datatype score 0.68. Evidence tier "clinical-evidence" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery 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.