+ |
PRKACA | down-regulates activity
phosphorylation
|
HMGCR |
0.338 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-249992 |
Ser872 |
SHMIHNRsKINLQDL |
Rattus norvegicus |
|
pmid |
sentence |
2369897 |
The intact, 100 kd microsomal enzyme and the 53 kd catalytic fragment of rat HMG-CoA reductase are both phosphorylated and inactivated by the AMP-activated protein kinase. this site is highly phosphorylated in intact liver under these conditions (Ser872 in the human enzyme). |
|
Publications: |
1 |
Organism: |
Rattus Norvegicus |
+ |
lovastatin | down-regulates activity
chemical inhibition
|
HMGCR |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-258351 |
|
|
in vitro |
|
pmid |
sentence |
1597859 |
A series of N-heteroaryl-substituted mevalonolactones were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase both in vitro and in vivo, and to lower plasma cholesterol in a hypercholesterolemic dog model. The goal of the strategy employed was to design an inhibitor which possessed the pharmacological properties of lovastatin (1), and the physicochemical properties (increased hydrophilicity) of pravastatin (2). |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-258403 |
|
|
in vitro |
|
pmid |
sentence |
6933445 |
Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent. |
|
Publications: |
2 |
Organism: |
In Vitro |
+ |
SYVN1 | down-regulates quantity by destabilization
polyubiquitination
|
HMGCR |
0.579 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-272594 |
|
|
Mus musculus |
NIH-3T3 Cell |
pmid |
sentence |
14593114 |
In the presence of the ubiquitin-conjugating enzyme UBC7, the RING-H2 finger has in vitro ubiquitination activity for Lys(48)-specific polyubiquitin linkage, suggesting that human HRD1 is an E3 ubiquitin ligase involved in protein degradation.Human HRD1 appears to be involved in the basal degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase but not in the degradation that is regulated by sterols. |
|
Publications: |
1 |
Organism: |
Mus Musculus |
+ |
Clinofibrate | down-regulates
chemical inhibition
|
HMGCR |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-191085 |
|
|
Homo sapiens |
|
pmid |
sentence |
Other |
|
|
Publications: |
1 |
Organism: |
Homo Sapiens |
+ |
pravastatin | down-regulates activity
chemical inhibition
|
HMGCR |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-258350 |
|
|
in vitro |
|
pmid |
sentence |
1597859 |
A series of N-heteroaryl-substituted mevalonolactones were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase both in vitro and in vivo, and to lower plasma cholesterol in a hypercholesterolemic dog model. The goal of the strategy employed was to design an inhibitor which possessed the pharmacological properties of lovastatin (1), and the physicochemical properties (increased hydrophilicity) of pravastatin (2). |
|
Publications: |
1 |
Organism: |
In Vitro |
+ |
SREBF2 | up-regulates quantity by expression
transcriptional regulation
|
HMGCR |
0.508 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-265161 |
|
|
Homo sapiens |
|
pmid |
sentence |
31848472 |
The processed SREBP2, designated nuclear SREBP2 (nSREBP2), then enters the nucleus as a homodimer, binds to the sterol regulatory element (SRE) sequence in the promoters of target genes, including HMGCR and SQLE (encoding squalene monooxygenase), and upregulates their transcription |
|
Publications: |
1 |
Organism: |
Homo Sapiens |
Tissue: |
Liver |
+ |
simvastatin | down-regulates activity
chemical inhibition
|
HMGCR |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-258348 |
|
|
in vitro |
|
pmid |
sentence |
1433193 |
Substitution of hydroxy and hydroxyalkyl functionality at C-7 of the hexahydronaphthalene nucleus of simvastatin has provided novel analogs. The synthetic strategy employed epoxidation or Lewis acid-catalyzed aldol reaction of the 8-keto silyl enol ether as a key reactive intermediate. These analogs were evaluated as potential hypocholesterolemic agents via initial determination of their ability to inhibit HMG-CoA reductase in vitro. |
|
Publications: |
1 |
Organism: |
In Vitro |