Page last updated: 2024-08-07 16:36:29
Squalene synthase
A squalene synthase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P37268]
Synonyms
SQS;
SS;
EC 2.5.1.21;
FPP:FPP farnesyltransferase;
Farnesyl-diphosphate farnesyltransferase;
Farnesyl-diphosphate farnesyltransferase 1
Research
Bioassay Publications (7)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (14.29) | 18.2507 |
| 2000's | 3 (42.86) | 29.6817 |
| 2010's | 3 (42.86) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (6)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| amiodarone | Homo sapiens (human) | IC50 | 8.0000 | 1 | 1 |
| b 581 | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
| sq 109 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sq 109 | Homo sapiens (human) | Ki | 0.7400 | 1 | 1 |
| tak 475 | Homo sapiens (human) | IC50 | 0.1455 | 2 | 2 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nadp | Homo sapiens (human) | Km | 430.0000 | 1 | 1 |
| farnesyl pyrophosphate | Homo sapiens (human) | Km | 2.3000 | 1 | 1 |
Multitarget drug discovery for tuberculosis and other infectious diseases.Journal of medicinal chemistry, , Apr-10, Volume: 57, Issue:7, 2014
Head-to-head prenyl tranferases: anti-infective drug targets.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
Identification of 4H,6H-[2]benzoxepino[4,5-c][1,2]oxazoles as novel squalene synthase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Synthesis of novel 4,1-benzoxazepine derivatives as squalene synthase inhibitors and their inhibition of cholesterol synthesis.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| farnesyltranstransferase activity | molecular function | Catalysis of the reaction: 2-trans,6-trans-farnesyl diphosphate + isopentenyl diphosphate = diphosphate + geranylgeranyl diphosphate. [EC:2.5.1.29, RHEA:17653] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| farnesyl-diphosphate farnesyltransferase activity | molecular function | Catalysis of the reaction: 2 farnesyl diphosphate = diphosphate + presqualene diphosphate. [EC:2.5.1.21] |
| squalene synthase activity | molecular function | Catalysis of the reaction: presqualene diphosphate + NADPH = squalene + NADP+ + diphosphate. [EC:2.5.1.21] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| 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] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
Involved In
This protein is involved in 3 target(s):
| Target | Category | Definition |
|---|
| steroid biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of steroids, compounds with a 1,2,cyclopentanoperhydrophenanthrene nucleus; includes de novo formation and steroid interconversion by modification. [GOC:go_curators] |
| farnesyl diphosphate metabolic process | biological process | The chemical reactions and pathways involving farnesyl diphosphate, an intermediate in carotenoid, sesquiterpene, squalene and sterol biosynthesis, as well as a substrate in protein farnesylation. [GOC:go_curators] |
| 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] |