Proteins > 3-hydroxy-3-methylglutaryl-coenzyme A reductase
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3-hydroxy-3-methylglutaryl-coenzyme A reductase
A 3-hydroxy-3-methylglutaryl-coenzyme A reductase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P04035]
Synonyms
HMG-CoA reductase;
EC 1.1.1.34
Research
Bioassay Publications (23)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (30.43) | 18.2507 |
| 2000's | 7 (30.43) | 29.6817 |
| 2010's | 7 (30.43) | 24.3611 |
| 2020's | 2 (8.70) | 2.80 |
Compounds (20)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Discovery of a new class of HMG-CoA reductase inhibitor from Polyalthia longifolia as potential lipid lowering agent.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
Synthesis and biological evaluation of dihydroeptastatin, a novel inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase.Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
Inhibitors of cholesterol biosynthesis. 6. trans-6-[2-(2-N-heteroaryl-3,5-disubstituted- pyrazol-4-yl)ethyl/ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones.Journal of medicinal chemistry, , May-29, Volume: 35, Issue:11, 1992
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 3. Lactones of 6-phenoxy-3,5-dihydroxyhexanoic acids.Journal of medicinal chemistry, , Volume: 34, Issue:10, 1991
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 1. Lactones of pyridine- and pyrimidine-substituted 3,5-dihydroxy-6-heptenoic (-heptanoic) acids.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 2. Derivatives of 7-(1H-pyrrol-3-yl)-substituted-3,5-dihydroxyhept-6(E)-enoic (-heptanoic) acids.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
[no title available],
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Synthesis and highly potent hypolipidemic activity of alpha-asarone- and fibrate-based 2-acyl and 2-alkyl phenols as HMG-CoA reductase inhibitors.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA).Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Molecular docking of the highly hypolipidemic agent alpha-asarone with the catalytic portion of HMG-CoA reductase.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
[no title available],
Lovastatin Analogues from the Soil-Derived Fungus Aspergillus sclerotiorum PSU-RSPG178.Journal of natural products, , 06-24, Volume: 79, Issue:6, 2016
Inhibitors of cholesterol biosynthesis. 6. trans-6-[2-(2-N-heteroaryl-3,5-disubstituted- pyrazol-4-yl)ethyl/ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones.Journal of medicinal chemistry, , May-29, Volume: 35, Issue:11, 1992
[no title available],
Why Some Targets Benefit from beyond Rule of Five Drugs.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA).Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
[no title available],
Why Some Targets Benefit from beyond Rule of Five Drugs.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA).Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 9. The synthesis and biological evaluation of novel simvastatin analogs.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
[no title available],
Luciferase-based HMG-CoA reductase degradation assay for activity and selectivity profiling of oxy(lano)sterols.Bioorganic & medicinal chemistry, , 02-01, Volume: 28, Issue:3, 2020
Design and synthesis of seco-oxysterol analogs as potential inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase gene transcription.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Bisphosphonate esters interact with HMG-CoA reductase membrane domain to induce its degradation.Bioorganic & medicinal chemistry, , 07-15, Volume: 28, Issue:14, 2020
Luciferase-based HMG-CoA reductase degradation assay for activity and selectivity profiling of oxy(lano)sterols.Bioorganic & medicinal chemistry, , 02-01, Volume: 28, Issue:3, 2020
Thermodynamic and structure guided design of statin based inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA).Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Molecular docking of the highly hypolipidemic agent alpha-asarone with the catalytic portion of HMG-CoA reductase.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Synthesis and biological evaluations of condensed pyridine and condensed pyrimidine-based HMG-CoA reductase inhibitors.Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
Inhibitors of cholesterol biosynthesis. 6. trans-6-[2-(2-N-heteroaryl-3,5-disubstituted- pyrazol-4-yl)ethyl/ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones.Journal of medicinal chemistry, , May-29, Volume: 35, Issue:11, 1992
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| hydroxymethylglutaryl-CoA reductase (NADPH) activity | molecular function | Catalysis of the reaction: (R)-mevalonate + CoA + 2 NADP+ = (S)-3-hydroxy-3-methylglutaryl-CoA + 2 H+ + 2 NADPH. [PMID:29224355, RHEA:15989] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| GTPase regulator activity | molecular function | Binds to and modulates the activity of a GTPase. [GOC:mah] |
| NADPH binding | molecular function | Binding to the reduced form, NADPH, of nicotinamide-adenine dinucleotide phosphate, a coenzyme involved in many redox and biosynthetic reactions. [GOC:mah] |
| coenzyme A binding | molecular function | Binding to coenzyme A, 3'-phosphoadenosine-(5')diphospho(4')pantatheine, an acyl carrier in many acylation and acyl-transfer reactions in which the intermediate is a thiol ester. [GOC:krc, ISBN:0198547684] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| peroxisomal membrane | cellular component | The lipid bilayer surrounding a peroxisome. [GOC:mah] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| peroxisomal membrane | cellular component | The lipid bilayer surrounding a peroxisome. [GOC:mah] |
Involved In
This protein is involved in 10 target(s):
| Target | Category | Definition |
|---|
| cholesterol biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of cholesterol, cholest-5-en-3 beta-ol, the principal sterol of vertebrates and the precursor of many steroids, including bile acids and steroid hormones. [GOC:ai] |
| visual learning | biological process | Any process in an organism in which a change in behavior of an individual occurs in response to repeated exposure to a visual cue. [GOC:jid, ISBN:0582227089] |
| coenzyme A metabolic process | biological process | The chemical reactions and pathways involving coenzyme A, 3'-phosphoadenosine-(5')diphospho(4')pantatheine, an acyl carrier in many acylation and acyl-transfer reactions in which the intermediate is a thiol ester. [ISBN:0198547684] |
| negative regulation of protein catabolic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of protein catabolic process. [GO_REF:0000058, GOC:kmv, GOC:obol, GOC:TermGenie, PMID:24785082] |
| negative regulation of protein secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the controlled release of a protein from a cell. [GOC:ai] |
| long-term synaptic potentiation | biological process | A process that modulates synaptic plasticity such that synapses are changed resulting in the increase in the rate, or frequency of synaptic transmission at the synapse. [GOC:dgh, GOC:dph] |
| regulation of ERK1 and ERK2 cascade | biological process | Any process that modulates the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:add, ISBN:0121245462, ISBN:0896039986] |
| negative regulation of amyloid-beta clearance | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of amyloid-beta clearance. [GOC:BHF, GOC:TermGenie] |
| isoprenoid biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of an isoprenoid compound, isoprene (2-methylbuta-1,3-diene) or compounds containing or derived from linked isoprene (3-methyl-2-butenylene) residues. [ISBN:0198506732] |
| sterol biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of sterols, steroids with one or more hydroxyl groups and a hydrocarbon side-chain in the molecule. [GOC:go_curators] |