Target Information
| Target General Information | Top | |||||
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| Target ID |
T56545
(Former ID: TTDI02020)
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| Target Name |
Apolipoprotein A-I (APOA1)
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| Synonyms |
Truncated apolipoprotein AI; Apolipoprotein A1; ApoAI; ApoA-I; Apo-AI
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| Gene Name |
APOA1
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Cardiovascular disease [ICD-11: BA00-BE2Z] | |||||
| 2 | Myocardial infarction [ICD-11: BA41-BA43] | |||||
| 3 | Aortic valve stenosis [ICD-11: BB70] | |||||
| 4 | Arterial occlusive disease [ICD-11: BD40] | |||||
| Function |
As part of the SPAP complex, activates spermatozoa motility. Participates in the reverse transport of cholesterol from tissues to the liver for excretion by promoting cholesterol efflux from tissues and by acting as a cofactor for the lecithin cholesterol acyltransferase (LCAT).
Click to Show/Hide
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| BioChemical Class |
Apolipoprotein
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| UniProt ID | ||||||
| Sequence |
MKAAVLTLAVLFLTGSQARHFWQQDEPPQSPWDRVKDLATVYVDVLKDSGRDYVSQFEGS
ALGKQLNLKLLDNWDSVTSTFSKLREQLGPVTQEFWDNLEKETEGLRQEMSKDLEEVKAK VQPYLDDFQKKWQEEMELYRQKVEPLRAELQEGARQKLHELQEKLSPLGEEMRDRARAHV DALRTHLAPYSDELRQRLAARLEALKENGGARLAEYHAKATEHLSTLSEKAKPALEDLRQ GLLPVLESFKVSFLSALEEYTKKLNTQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T44S1A | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
| 1 | CER-001 | Drug Info | Phase 2 | Acute coronary syndrome | [2] | |
| 2 | CSL-112 | Drug Info | Phase 2 | Arteriosclerosis | [3] | |
| 3 | CER-522 | Drug Info | Phase 1 | Aortic valve stenosis | [4] | |
| 4 | MDCO-216 | Drug Info | Phase 1 | Arteriosclerosis | [5] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | CRD-5 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [6] | |
| 2 | APP-018 | Drug Info | Discontinued in Phase 1 | Arteriosclerosis | [7] | |
| 3 | AMT-050 | Drug Info | Terminated | Cholesterol metabolism disorder | [8] | |
| 4 | LSI-518P | Drug Info | Terminated | Cardiovascular disease | [9] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 7 Modulator drugs | + | ||||
| 1 | CER-001 | Drug Info | [10] | |||
| 2 | CSL-112 | Drug Info | [1] | |||
| 3 | CER-522 | Drug Info | [11] | |||
| 4 | MDCO-216 | Drug Info | [12] | |||
| 5 | APP-018 | Drug Info | [14] | |||
| 6 | AMT-050 | Drug Info | [15] | |||
| 7 | LSI-518P | Drug Info | [16] | |||
| Stimulator | [+] 1 Stimulator drugs | + | ||||
| 1 | CRD-5 | Drug Info | [13] | |||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating Transcription Factors | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | CER-001, a HDL-mimetic, stimulates the reverse lipid transport and atherosclerosis regression in high cholesterol diet-fed LDL-receptor deficient mice. Atherosclerosis. 2014 Jan;232(1):110-8. | |||||
| REF 2 | ClinicalTrials.gov (NCT01412034) Effect of CER-001 on Plaque Volume in Homozygous Familial Hypercholesterolemia (HoFH) Subjects. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT02108262) A Phase 2b Study of CSL112 in Subjects With Acute Myocardial Infarction.. U.S. National Institutes of Health. | |||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033541) | |||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012886) | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021641) | |||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022118) | |||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026835) | |||||
| REF 9 | HDL mimetic peptide ATI-5261 forms an oligomeric assembly in solution that dissociates to monomers upon dilution. Biochemistry. 2011 May 17;50(19):4068-76. | |||||
| REF 10 | Clinical pipeline report, company report or official report of Cerenis. | |||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033541) | |||||
| REF 12 | MDCO-216 (Apo A-I Milano/POPC Complex) Administered to Cynomolgus Monkeys Induces Pronounced Changes in Plasma Lipids and Apolipoproteins. Circulation. 2011; 124: A10978. | |||||
| REF 13 | Emerging antidyslipidemic drugs. Expert Opin Emerg Drugs. 2008 Jun;13(2):363-81. | |||||
| REF 14 | Apolipoprotein A-I and its mimetics for the treatment of atherosclerosis. Curr Opin Investig Drugs. 2010 September; 11(9): 989-996. | |||||
| REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026835) | |||||
| REF 16 | Clinical review: The evolving role of HDL in the treatment of high-risk patients with cardiovascular disease. J Clin Endocrinol Metab. 2011 May;96(5):1246-57. | |||||
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