Details of the Drug Transporter (DTP)

General Information of Drug Transporter (DTP) (ID: DT61TWI)

DTP Name ATP-binding cassette sub-family A member 1 (ABCA1)
Gene Name ABCA1
UniProt ID
O95477 (ABCA1_HUMAN)
VARIDT ID
DTD0036
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Synonyms ABC-1; ABC1; ABCA1; ATP-binding cassette 1; ATP-binding cassette transporter 1; CERP; Cholesterol efflux regulatory protein; HDLDT1; TGD
DTP Family ATP-Binding Cassette (ABC) Superfamily
Cholesterol/Phospholipid/Retinal (CPR) Flippase Family (ABCA)
Tissue Specificity Widely expressed, but most abundant inmacrophages.
Sequence
MACWPQLRLLLWKNLTFRRRQTCQLLLEVAWPLFIFLILISVRLSYPPYEQHECHFPNKA
MPSAGTLPWVQGIICNANNPCFRYPTPGEAPGVVGNFNKSIVARLFSDARRLLLYSQKDT
SMKDMRKVLRTLQQIKKSSSNLKLQDFLVDNETFSGFLYHNLSLPKSTVDKMLRADVILH
KVFLQGYQLHLTSLCNGSKSEEMIQLGDQEVSELCGLPREKLAAAERVLRSNMDILKPIL
RTLNSTSPFPSKELAEATKTLLHSLGTLAQELFSMRSWSDMRQEVMFLTNVNSSSSSTQI
YQAVSRIVCGHPEGGGLKIKSLNWYEDNNYKALFGGNGTEEDAETFYDNSTTPYCNDLMK
NLESSPLSRIIWKALKPLLVGKILYTPDTPATRQVMAEVNKTFQELAVFHDLEGMWEELS
PKIWTFMENSQEMDLVRMLLDSRDNDHFWEQQLDGLDWTAQDIVAFLAKHPEDVQSSNGS
VYTWREAFNETNQAIRTISRFMECVNLNKLEPIATEVWLINKSMELLDERKFWAGIVFTG
ITPGSIELPHHVKYKIRMDIDNVERTNKIKDGYWDPGPRADPFEDMRYVWGGFAYLQDVV
EQAIIRVLTGTEKKTGVYMQQMPYPCYVDDIFLRVMSRSMPLFMTLAWIYSVAVIIKGIV
YEKEARLKETMRIMGLDNSILWFSWFISSLIPLLVSAGLLVVILKLGNLLPYSDPSVVFV
FLSVFAVVTILQCFLISTLFSRANLAAACGGIIYFTLYLPYVLCVAWQDYVGFTLKIFAS
LLSPVAFGFGCEYFALFEEQGIGVQWDNLFESPVEEDGFNLTTSVSMMLFDTFLYGVMTW
YIEAVFPGQYGIPRPWYFPCTKSYWFGEESDEKSHPGSNQKRISEICMEEEPTHLKLGVS
IQNLVKVYRDGMKVAVDGLALNFYEGQITSFLGHNGAGKTTTMSILTGLFPPTSGTAYIL
GKDIRSEMSTIRQNLGVCPQHNVLFDMLTVEEHIWFYARLKGLSEKHVKAEMEQMALDVG
LPSSKLKSKTSQLSGGMQRKLSVALAFVGGSKVVILDEPTAGVDPYSRRGIWELLLKYRQ
GRTIILSTHHMDEADVLGDRIAIISHGKLCCVGSSLFLKNQLGTGYYLTLVKKDVESSLS
SCRNSSSTVSYLKKEDSVSQSSSDAGLGSDHESDTLTIDVSAISNLIRKHVSEARLVEDI
GHELTYVLPYEAAKEGAFVELFHEIDDRLSDLGISSYGISETTLEEIFLKVAEESGVDAE
TSDGTLPARRNRRAFGDKQSCLRPFTEDDAADPNDSDIDPESRETDLLSGMDGKGSYQVK
GWKLTQQQFVALLWKRLLIARRSRKGFFAQIVLPAVFVCIALVFSLIVPPFGKYPSLELQ
PWMYNEQYTFVSNDAPEDTGTLELLNALTKDPGFGTRCMEGNPIPDTPCQAGEEEWTTAP
VPQTIMDLFQNGNWTMQNPSPACQCSSDKIKKMLPVCPPGAGGLPPPQRKQNTADILQDL
TGRNISDYLVKTYVQIIAKSLKNKIWVNEFRYGGFSLGVSNTQALPPSQEVNDAIKQMKK
HLKLAKDSSADRFLNSLGRFMTGLDTKNNVKVWFNNKGWHAISSFLNVINNAILRANLQK
GENPSHYGITAFNHPLNLTKQQLSEVALMTTSVDVLVSICVIFAMSFVPASFVVFLIQER
VSKAKHLQFISGVKPVIYWLSNFVWDMCNYVVPATLVIIIFICFQQKSYVSSTNLPVLAL
LLLLYGWSITPLMYPASFVFKIPSTAYVVLTSVNLFIGINGSVATFVLELFTDNKLNNIN
DILKSVFLIFPHFCLGRGLIDMVKNQAMADALERFGENRFVSPLSWDLVGRNLFAMAVEG
VVFFLITVLIQYRFFIRPRPVNAKLSPLNDEDEDVRRERQRILDGGGQNDILEIKELTKI
YRRKRKPAVDRICVGIPPGECFGLLGVNGAGKSSTFKMLTGDTTVTRGDAFLNKNSILSN
IHEVHQNMGYCPQFDAITELLTGREHVEFFALLRGVPEKEVGKVGEWAIRKLGLVKYGEK
YAGNYSGGNKRKLSTAMALIGGPPVVFLDEPTTGMDPKARRFLWNCALSVVKEGRSVVLT
SHSMEECEALCTRMAIMVNGRFRCLGSVQHLKNRFGDGYTIVVRIAGSNPDLKPVQDFFG
LAFPGSVLKEKHRNMLQYQLPSSLSSLARIFSILSQSKKRLHIEDYSVSQTTLDQVFVNF
AKDQSDDDHLKDLSLHKNQTVVDVAVLTSFLQDEKVKESYV
Function
This transporter is cAMP-dependent and sulfonylurea-sensitive. Involved in the efflux of intracellular cholesterol and phospholipids and their transfer to apoliproteins to form nascent high density lipoproteins/HDLs.
Endogenous Substrate(s) Lipids
TCDB ID
3.A.1.211.14
Gene ID
19
KEGG Pathway
ABC transporters (hsa02010 )
Fat digestion and absorption (hsa04975 )
Cholesterol metabolism (hsa04979 )
Lipid and atherosclerosis (hsa05417 )
Reactome Pathway
Defective ABCA1 causes TGD (R-HSA-5682113 )
HDL assembly (R-HSA-8963896 )
NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux (R-HSA-9029569 )
PPARA activates gene expression (R-HSA-1989781 )

Molecular Interaction Atlas (MIA) of This DTP

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTP
1 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
FENOFIBRIC ACID DMGO2MC Cardiovascular disease BA00-BE2Z Approved [4]
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1 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cholesterol DMR3J6S Discovery agent N.A. Investigative [5]
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Molecular Expression Atlas (MEA) of This DTP

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTP
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 4.76E-05 4.28E-01 5.57E-01
Adrenocortical carcinoma 2D11.Z Kidney 1.53E-03 -6.39E-01 -1.09E+00
Alopecia ED70 Skin from scalp 1.30E-03 1.37E-01 5.21E-01
Alzheimer's disease 8A20 Entorhinal cortex 4.68E-05 1.30E-01 2.97E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 1.82E-01 -1.02E-01 -2.78E-01
Aortic stenosis BB70 Calcified aortic valve 5.69E-01 8.68E-02 2.96E-01
Apnea 7A40 Hyperplastic tonsil 1.10E-01 -3.20E-01 -9.19E-01
Arthropathy FA00-FA5Z Peripheral blood 5.05E-03 4.23E-01 1.34E+00
Asthma CA23 Nasal and bronchial airway 2.61E-06 4.19E-01 6.42E-01
Atopic dermatitis EA80 Skin 1.75E-01 -4.79E-02 -1.20E-01
Autism 6A02 Whole blood 8.79E-01 -6.06E-02 -1.84E-01
Autoimmune uveitis 9A96 Peripheral monocyte 4.09E-01 -2.33E-01 -1.51E-01
Autosomal dominant monocytopenia 4B04 Whole blood 1.09E-02 1.36E+00 2.75E+00
Bacterial infection of gingival 1C1H Gingival tissue 2.93E-05 2.03E-01 7.79E-01
Batten disease 5C56.1 Whole blood 5.29E-01 3.62E-02 2.00E-01
Behcet's disease 4A62 Peripheral blood 4.59E-01 6.64E-02 2.36E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 4.32E-01 8.31E-02 2.31E-01
Bladder cancer 2C94 Bladder tissue 5.39E-08 -4.98E-01 -3.90E+00
Breast cancer 2C60-2C6Z Breast tissue 2.11E-16 -2.22E-01 -4.63E-01
Cardioembolic stroke 8B11.20 Whole blood 1.62E-08 6.03E-01 1.45E+00
Cervical cancer 2C77 Cervical tissue 4.24E-01 7.38E-02 2.00E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 9.94E-01 8.22E-02 7.66E-02
Chronic hepatitis C 1E51.1 Whole blood 7.13E-01 -1.46E-01 -1.24E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 6.17E-02 -1.81E-01 -7.21E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 5.41E-01 -2.94E-03 -7.55E-03
Chronic rhinosinusitis CA0A Sinus mucosa tissue 6.00E-02 3.48E-01 8.51E-01
Colon cancer 2B90 Colon tissue 1.91E-21 -2.91E-01 -8.95E-01
Coronary artery disease BA80-BA8Z Peripheral blood 4.88E-01 -9.63E-02 -3.33E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 9.14E-01 6.39E-02 3.32E-01
Endometriosis GA10 Endometrium tissue 1.21E-03 3.52E-01 7.12E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 3.77E-01 5.71E-02 2.68E-01
Familial hypercholesterolemia 5C80.00 Whole blood 2.58E-02 -3.34E-01 -9.69E-01
Gastric cancer 2B72 Gastric tissue 6.18E-01 8.11E-02 5.65E-01
Glioblastopma 2A00.00 Nervous tissue 2.76E-167 1.26E+00 2.43E+00
Glioma 2A00.0Y-2A00.0Z White matter tissue 4.58E-02 2.93E-01 5.98E-01
Head and neck cancer 2D42 Head and neck tissue 1.31E-31 9.16E-01 1.75E+00
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 3.16E-01 1.16E-01 2.47E-01
Huntington's disease 8A01.10 Whole blood 3.54E-01 1.39E-01 5.02E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 4.22E-01 -7.61E-02 -1.81E-01
Immunodeficiency 4A00-4A20 Peripheral blood 3.36E-03 9.23E-02 8.38E-01
Influenza 1.00E+30 Whole blood 7.21E-03 -5.80E-01 -4.31E+00
Interstitial cystitis GC00.3 Bladder tissue 5.61E-01 -7.23E-02 -6.35E-01
Intracranial aneurysm 8B01.0 Intracranial artery 1.29E-02 5.31E-01 1.32E+00
Irritable bowel syndrome DD91.0 Rectal colon tissue 7.00E-01 -4.01E-02 -1.32E-01
Ischemic stroke 8B11 Peripheral blood 3.20E-01 3.47E-01 6.86E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 1.05E-04 2.06E-01 4.78E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 3.73E-01 9.66E-02 3.48E-01
Lateral sclerosis 8B60.4 Skin 1.19E-01 -1.75E-01 -3.98E+00
Liver cancer 2C12.0 Liver tissue 9.87E-05 -3.83E-01 -8.20E-01
Liver failure DB99.7-DB99.8 Liver tissue 3.86E-02 -6.52E-01 -2.23E+00
Lung cancer 2C25 Lung tissue 2.88E-05 -1.42E-01 -3.98E-01
Lupus erythematosus 4A40 Whole blood 2.15E-12 5.08E-01 8.17E-01
Major depressive disorder 6A70-6A7Z Whole blood 7.95E-01 2.12E-02 6.53E-02
Major depressive disorder 6A70-6A7Z Hippocampus 7.65E-01 -2.02E-02 -6.13E-02
Melanoma 2C30 Skin 8.93E-02 3.78E-01 6.24E-01
Multiple myeloma 2A83.1 Bone marrow 1.36E-01 -2.13E-01 -3.79E-01
Multiple myeloma 2A83.1 Peripheral blood 9.00E-01 -9.52E-03 -6.03E-02
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 1.45E-01 2.26E-01 9.70E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 2.20E-01 2.39E-03 2.81E-03
Myelofibrosis 2A20.2 Whole blood 1.04E-01 2.30E-01 9.92E-01
Myocardial infarction BA41-BA50 Peripheral blood 1.76E-08 1.04E+00 1.45E+00
Myopathy 8C70.6 Muscle tissue 3.04E-04 5.18E-01 2.02E+00
Neonatal sepsis KA60 Whole blood 1.97E-11 5.13E-01 1.13E+00
Neuroectodermal tumour 2A00.11 Brain stem tissue 3.58E-01 6.57E-02 2.08E-01
Non-alcoholic fatty liver disease DB92 Liver tissue 5.11E-02 3.57E-01 8.44E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 4.10E-01 -3.09E-02 -3.61E-02
Olive pollen allergy CA08.00 Peripheral blood 9.21E-01 1.41E-01 2.23E-01
Oral cancer 2B6E Oral tissue 1.26E-05 7.89E-01 1.45E+00
Osteoarthritis FA00-FA0Z Synovial tissue 8.94E-01 9.43E-02 1.55E-01
Osteoporosis FB83.1 Bone marrow 2.11E-01 2.64E-01 6.34E-01
Ovarian cancer 2C73 Ovarian tissue 7.87E-01 -1.62E-01 -2.86E-01
Pancreatic cancer 2C10 Pancreas 5.27E-02 6.00E-01 9.15E-01
Parkinson's disease 8A00.0 Substantia nigra tissue 6.39E-01 3.00E-01 6.04E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 6.36E-02 1.82E-01 8.01E-01
Pituitary cancer 2D12 Pituitary tissue 3.96E-01 2.42E-01 8.68E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 9.16E-01 -9.99E-02 -4.13E-01
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 9.13E-01 -8.43E-02 -2.97E-01
Polycythemia vera 2A20.4 Whole blood 1.76E-05 4.23E-01 1.75E+00
Pompe disease 5C51.3 Biceps muscle 8.81E-02 -3.01E-01 -1.16E+00
Preterm birth KA21.4Z Myometrium 9.86E-01 -4.76E-01 -5.03E-01
Prostate cancer 2C82 Prostate 3.12E-01 -1.30E-01 -2.52E-01
Psoriasis EA90 Skin 9.11E-01 5.32E-02 1.42E-01
Rectal cancer 2B92 Rectal colon tissue 3.31E-01 -1.38E-01 -4.81E-01
Renal cancer 2C90-2C91 Kidney 2.70E-06 7.53E-01 2.62E+00
Retinoblastoma 2D02.2 Uvea 1.74E-08 1.67E+00 3.59E+00
Rheumatoid arthritis FA20 Synovial tissue 3.66E-02 3.09E-01 1.06E+00
Rhinovirus infection CA42.1 Nasal epithelium tissue 1.25E-01 9.46E-02 2.86E-01
Schizophrenia 6A20 Prefrontal cortex 3.28E-02 1.12E-01 3.57E-01
Schizophrenia 6A20 Superior temporal cortex 1.26E-01 2.46E-01 8.82E-01
Scleroderma 4A42.Z Whole blood 1.04E-05 4.19E-01 2.59E+00
Seizure 8A60-8A6Z Whole blood 7.44E-01 2.84E-01 4.30E-01
Sensitive skin EK0Z Skin 2.78E-01 -6.01E-02 -4.70E-01
Sepsis with septic shock 1G41 Whole blood 1.14E-38 5.74E-01 1.37E+00
Shwachman-Diamond syndrome 3A70.0 Bone marrow 3.95E-01 -2.67E-02 -1.00E-01
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 4.96E-02 -1.38E-01 -1.27E+00
Simpson golabi behmel syndrome LD2C Adipose tissue 7.91E-01 2.70E-01 9.09E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 1.09E-01 4.12E-01 1.69E+00
Skin cancer 2C30-2C3Z Skin 1.48E-06 -1.93E-01 -4.71E-01
Thrombocythemia 3B63 Whole blood 6.56E-01 -4.00E-02 -1.72E-01
Thrombocytopenia 3B64 Whole blood 8.57E-01 1.03E-01 3.51E-01
Thyroid cancer 2D10 Thyroid 2.56E-30 4.82E-01 1.61E+00
Tibial muscular dystrophy 8C75 Muscle tissue 6.00E-01 -1.77E-01 -2.43E-01
Tuberous sclerosis complex LD2D.2 Perituberal tissue 4.68E-03 6.77E-01 2.98E+00
Type 2 diabetes 5A11 Liver tissue 3.79E-02 4.70E-01 2.16E+00
Ureter cancer 2C92 Urothelium 8.48E-01 1.61E-02 8.66E-02
Uterine cancer 2C78 Endometrium tissue 1.58E-01 9.12E-02 1.78E-01
Vitiligo ED63.0 Skin 8.66E-01 -2.07E-02 -7.99E-02
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⏷ Show the Full List of Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DTP

DTP DTT Name ATP-binding cassette transporter A1 (ABCA1) DTT Info
DTP DTT Type Successful
1 Approved Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Probucol DMVZQ2M Coronary artery disease BA80 Approved [1]
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1 Discontinued Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
RG-7273 DMXMQAT Lipid metabolism disorder 5C52.Z Discontinued in Phase 1 [2]
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1 Investigative Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
RG7232 DMSTL12 Dyslipidemia 5C80-5C81 Investigative [3]
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References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 756).
3 Analysis of "On/Off" Kinetics of a CETP Inhibitor Using a Mechanistic Model of Lipoprotein Metabolism and Kinetics. CPT Pharmacometrics Syst Pharmacol. 2015 Aug;4(8):465-73.
4 Fenofibric acid, an active form of fenofibrate, increases apolipoprotein A-I-mediated high-density lipoprotein biogenesis by enhancing transcription of ATP-binding cassette transporter A1 gene in a liver X receptor-dependent manner. Arterioscler Thromb Vasc Biol. 2005 Jun;25(6):1193-7.
5 ABCA1 redistributes membrane cholesterol independent of apolipoprotein interactions. J Lipid Res. 2003 Jul;44(7):1373-80.