Target Information

Target General Infomation
Target ID
T56545
Former ID
TTDI02020
Target Name
Apolipoprotein A-I
Gene Name
APOA1
Synonyms
ApoAI; Apolipoprotein A1; Truncated apolipoprotein AI; APOA1
Target Type
Clinical Trial
Disease Atherosclerosis [ICD9: 414.0, 440; ICD10: I70]
Aortic valve stenosis [ICD10: I35.0, I06.0]
Acute coronary syndrome [ICD9: 444; ICD10: I74]
Cardiovascular disorder [ICD10: I00-I99]
Cholesterol metabolism disorder [ICD10: E70-E88]
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Function
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). As part of the SPAPcomplex, activates spermatozoa motility.
BioChemical Class
Apolipoprotein
UniProt ID
P02647
Sequence
MKAAVLTLAVLFLTGSQARHFWQQDEPPQSPWDRVKDLATVYVDVLKDSGRDYVSQFEGS
ALGKQLNLKLLDNWDSVTSTFSKLREQLGPVTQEFWDNLEKETEGLRQEMSKDLEEVKAK
VQPYLDDFQKKWQEEMELYRQKVEPLRAELQEGARQKLHELQEKLSPLGEEMRDRARAHV
DALRTHLAPYSDELRQRLAARLEALKENGGARLAEYHAKATEHLSTLSEKAKPALEDLRQ
GLLPVLESFKVSFLSALEEYTKKLNTQ
Drugs and Mode of Action
Drug(s) CER-001 Drug Info Phase 2 Acute coronary syndrome [523582]
CSL-112 Drug Info Phase 2 Atherosclerosis [524706]
CER-522 Drug Info Phase 1 Aortic valve stenosis [549195]
MDCO-216 Drug Info Phase 1 Atherosclerosis [547079]
MDCO-216 Drug Info Preclinical Acute coronary syndrome [547079]
CRD-5 Drug Info Discontinued in Phase 2 Hyperlipidaemia [548068]
APP-018 Drug Info Discontinued in Phase 1 Atherosclerosis [548120]
AMT-050 Drug Info Terminated Cholesterol metabolism disorder [548587]
LSI-518P Drug Info Terminated Cardiovascular disorder [531429]
Modulator AMT-050 Drug Info [548588]
APP-018 Drug Info [544167]
CER-001 Drug Info [550544]
CER-522 Drug Info [549196]
CSL-112 Drug Info [532615]
LSI-518P Drug Info [531385]
MDCO-216 Drug Info [551851]
Stimulator CRD-5 Drug Info [536740]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway PPAR signaling pathway
Fat digestion and absorption
Vitamin digestion and absorption
African trypanosomiasis
NetPath Pathway TGF_beta_Receptor Signaling Pathway
TNFalpha Signaling Pathway
Pathway Interaction Database FOXA2 and FOXA3 transcription factor networks
Reactome Platelet degranulation
ABC transporters in lipid homeostasis
Chylomicron-mediated lipid transport
HDL-mediated lipid transport
PPARA activates gene expression
Scavenging of heme from plasma
Scavenging by Class B Receptors
Scavenging by Class A Receptors
Retinoid metabolism and transport
Amyloid formation
WikiPathways Statin Pathway
Nuclear Receptors Meta-Pathway
PPAR Alpha Pathway
Human Complement System
Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
Binding and Uptake of Ligands by Scavenger Receptors
Visual phototransduction
Lipid digestion, mobilization, and transport
ABC-family proteins mediated transport
Folate Metabolism
Vitamin B12 Metabolism
Selenium Micronutrient Network
References
Ref 523582ClinicalTrials.gov (NCT01412034) Effect of CER-001 on Plaque Volume in Homozygous Familial Hypercholesterolemia (HoFH) Subjects. U.S. National Institutes of Health.
Ref 524706ClinicalTrials.gov (NCT02108262) A Phase 2b Study of CSL112 in Subjects With Acute Myocardial Infarction.. U.S. National Institutes of Health.
Ref 531429HDL 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 547079Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012886)
Ref 548068Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021641)
Ref 548120Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022118)
Ref 548587Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026835)
Ref 549195Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033541)
Ref 531385Clinical 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.
Ref 532615CER-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 536740Emerging antidyslipidemic drugs. Expert Opin Emerg Drugs. 2008 Jun;13(2):363-81.
Ref 544167Apolipoprotein A-I and its mimetics for the treatment of atherosclerosis. Curr Opin Investig Drugs. 2010 September; 11(9): 989-996.
Ref 548588Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026835)
Ref 549196Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033541)
Ref 550544Clinical pipeline report, company report or official report of Cerenis.
Ref 551851MDCO-216 (Apo A-I Milano/POPC Complex) Administered to Cynomolgus Monkeys Induces Pronounced Changes in Plasma Lipids and Apolipoproteins. Circulation. 2011; 124: A10978.

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