Target Information
| Target General Information | Top | |||||
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| Target ID |
T86115
(Former ID: TTDC00328)
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| Target Name |
ApoC-III messenger RNA (APOC3 mRNA)
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| Synonyms |
Apolipoprotein CIII (mRNA); Apolipoprotein C3 (mRNA); Apolipoprotein C-III (mRNA); ApoC-III (mRNA); Apo-CIII (mRNA)
Click to Show/Hide
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| Gene Name |
APOC3
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Hyper-lipoproteinaemia [ICD-11: 5C80] | |||||
| Function |
Plays a multifaceted role in triglyceride homeostasis. Intracellularly, promotes hepatic very low density lipoprotein 1 (VLDL1) assembly and secretion; extracellularly, attenuates hydrolysis and clearance of triglyceride-rich lipoproteins (TRLs). Impairs the lipolysis of TRLs by inhibiting lipoprotein lipase and the hepatic uptake of TRLs by remnant receptors. Formed of several curved helices connected via semiflexible hinges, so that it can wrap tightly around the curved micelle surface and easily adapt to the different diameters of its natural binding partners. Component of triglyceride-rich very low density lipoproteins (VLDL) and high density lipoproteins (HDL) in plasma.
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| BioChemical Class |
mRNA target
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| UniProt ID | ||||||
| Sequence |
MQPRVLLVVALLALLASARASEAEDASLLSFMQGYMKHATKTAKDALSSVQESQVAQQAR
GWVTDGFSSLKDYWSTVKDKFSEFWDLDPEVRPTSAVAA Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Volanesorsen | Drug Info | Approved | Hypertriglyceridemia | [2] | |
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | ARO-APOC3 | Drug Info | Phase 3 | Familial chylomicronemia syndrome | [3] | |
| 2 | Olezarsen | Drug Info | Phase 3 | Familial chylomicronemia syndrome | [4] | |
| 3 | ISIS-APOCIII | Drug Info | Phase 1 | Metabolic syndrome x | [1] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 3 Inhibitor drugs | + | ||||
| 1 | Volanesorsen | Drug Info | [2] | |||
| 2 | ARO-APOC3 | Drug Info | [5] | |||
| 3 | Olezarsen | Drug Info | [6] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | PPAR signaling pathway | |||||
| Reactome | [+] 3 Reactome Pathways | + | ||||
| 1 | Chylomicron-mediated lipid transport | |||||
| 2 | HDL-mediated lipid transport | |||||
| 3 | Retinoid metabolism and transport | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | Statin Pathway | |||||
| 2 | PPAR Alpha Pathway | |||||
| 3 | Visual phototransduction | |||||
| 4 | Lipid digestion, mobilization, and transport | |||||
| References | Top | |||||
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| REF 1 | Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2011). | |||||
| REF 2 | Metabolism and Disposition of Volanesorsen, a 2'- O-(2 methoxyethyl) Antisense Oligonucleotide, Across Species. Drug Metab Dispos. 2019 Oct;47(10):1164-1173. | |||||
| REF 3 | ClinicalTrials.gov (NCT05089084) A Phase 3 Study to Evaluate the Efficacy and Safety of ARO-APOC3 in Adults With Familial Chylomicronemia Syndrome. U.S.National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT05130450) An Open-Label Extension Study of AKCEA-APOCIII-LRx Administered Subcutaneously to Patients With Familial Chylomicronemia Syndrome (FCS). U.S.National Institutes of Health. | |||||
| REF 5 | ANGPTL3 and Apolipoprotein C-III as Novel Lipid-Lowering Targets. Curr Atheroscler Rep. 2021 Mar 10;23(5):20. | |||||
| REF 6 | Apolipoprotein C-III reduction in subjects with moderate hypertriglyceridaemia and at high cardiovascular risk. Eur Heart J. 2022 Apr 6;43(14):1401-1412. | |||||
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