Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT94G6BQ)

• DOT Name: Phospholipid-transporting ATPase ABCA1 (ABCA1)
• Synonyms: EC 7.6.2.1; ATP-binding cassette sub-family A member 1; ATP-binding cassette transporter 1; ABC-1; ATP-binding cassette 1; Cholesterol efflux regulatory protein
• Gene Name: ABCA1
• Related Disease:
  Hypoalphalipoproteinemia, primary, 1
  Tangier disease
  Obsolete apolipoprotein A-I deficiency
• UniProt ID: ABCA1_HUMAN
• PDB ID: 5XJY; 7ROQ; 7TBW; 7TBY; 7TBZ; 7TC0; 7TDT
• EC Number: 7.6.2.1
• Pfam ID: PF12698 ; PF00005
• 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: Catalyzes the translocation of specific phospholipids from the cytoplasmic to the extracellular/lumenal leaflet of membrane coupled to the hydrolysis of ATP. Thereby, participates in phospholipid transfer to apolipoproteins to form nascent high density lipoproteins/HDLs. Transports preferentially phosphatidylcholine over phosphatidylserine. May play a similar role in the efflux of intracellular cholesterol to apolipoproteins and the formation of nascent high density lipoproteins/HDLs. Translocates phospholipids from the outer face of the plasma membrane and forces it through its gateway and annulus into an elongated hydrophobic tunnel in its extracellular domain.
• Tissue Specificity: Widely expressed, but most abundant in macrophages.
• KEGG Pathway:
  ABC transporters (hsa02010)
  Efferocytosis (hsa04148)
  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 DOT

3 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Hypoalphalipoproteinemia, primary, 1	DIS9ENQR	Definitive	Autosomal dominant	[1]
Tangier disease	DIS57P0M	Definitive	Autosomal recessive	[2]
Obsolete apolipoprotein A-I deficiency	DIS4M8L1	Supportive	Autosomal dominant	[3]

This DOT Affected the Drug Response of 3 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Arsenic	DMTL2Y1	Approved	Phospholipid-transporting ATPase ABCA1 (ABCA1) affects the response to substance of Arsenic.	[60]
Mitoxantrone	DMM39BF	Approved	Phospholipid-transporting ATPase ABCA1 (ABCA1) affects the response to substance of Mitoxantrone.	[61]
Thalidomide	DM70BU5	Approved	Phospholipid-transporting ATPase ABCA1 (ABCA1) increases the response to substance of Thalidomide.	[62]

This DOT Affected the Regulation of Drug Effects of 1 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
ANW-32821	DMMJOZD	Phase 2	Phospholipid-transporting ATPase ABCA1 (ABCA1) increases the export of ANW-32821.	[63]

1 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the methylation of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[4]

69 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[5]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[6]
Acetaminophen	DMUIE76	Approved	Acetaminophen decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[7]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[8]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[5]
Quercetin	DM3NC4M	Approved	Quercetin decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[9]
Temozolomide	DMKECZD	Approved	Temozolomide decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[10]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[11]
Calcitriol	DM8ZVJ7	Approved	Calcitriol increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[12]
Vorinostat	DMWMPD4	Approved	Vorinostat decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[13]
Testosterone	DM7HUNW	Approved	Testosterone increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[14]
Carbamazepine	DMZOLBI	Approved	Carbamazepine affects the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[15]
Methotrexate	DM2TEOL	Approved	Methotrexate increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[16]
Folic acid	DMEMBJC	Approved	Folic acid increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[17]
Troglitazone	DM3VFPD	Approved	Troglitazone increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[18]
Rosiglitazone	DMILWZR	Approved	Rosiglitazone increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[19]
Ethanol	DMDRQZU	Approved	Ethanol decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[20]
Aspirin	DM672AH	Approved	Aspirin decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[21]
Nicotine	DMWX5CO	Approved	Nicotine decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[22]
Dasatinib	DMJV2EK	Approved	Dasatinib increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[23]
Simvastatin	DM30SGU	Approved	Simvastatin decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[24]
Obeticholic acid	DM3Q1SM	Approved	Obeticholic acid decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[25]
Fenofibrate	DMFKXDY	Approved	Fenofibrate increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[26]
Rifampicin	DM5DSFZ	Approved	Rifampicin decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[27]
Palbociclib	DMD7L94	Approved	Palbociclib increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[28]
Pioglitazone	DMKJ485	Approved	Pioglitazone increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[29]
Lindane	DMB8CNL	Approved	Lindane increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[30]
Fluoxetine	DM3PD2C	Approved	Fluoxetine decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[31]
Lovastatin	DM9OZWQ	Approved	Lovastatin increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[32]
Bezafibrate	DMZDCS0	Approved	Bezafibrate increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[26]
Omeprazole	DM471KJ	Approved	Omeprazole increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[33]
Clofibrate	DMPC1J7	Approved	Clofibrate increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[34]
Vitamin B3	DMQVRZH	Approved	Vitamin B3 increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[21]
Lansoprazole	DMXYLQ3	Approved	Lansoprazole increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[33]
Gemfibrozil	DMD8Q3J	Approved	Gemfibrozil increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[26]
Ezetimibe	DM7A8TW	Approved	Ezetimibe decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[35]
Pitavastatin	DMJH792	Approved	Pitavastatin increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[34]
Pantoprazole	DMSVOCZ	Approved	Pantoprazole increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[33]
Resveratrol	DM3RWXL	Phase 3	Resveratrol increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[36]
Epigallocatechin gallate	DMCGWBJ	Phase 3	Epigallocatechin gallate increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[37]
Atorvastatin	DMF28YC	Phase 3 Trial	Atorvastatin decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[19]
Genistein	DM0JETC	Phase 2/3	Genistein increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[38]
Amiodarone	DMUTEX3	Phase 2/3 Trial	Amiodarone decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[39]
GSK2110183	DMZHB37	Phase 2	GSK2110183 decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[40]
LY-518674	DMBM2I9	Phase 2	LY-518674 increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[26]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[5]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[41]
GSK618334	DMJPXZ4	Phase 1	GSK618334 increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[42]
BUTYLATEDHYDROXYTOLUENE	DMJ56MS	Phase 1	BUTYLATEDHYDROXYTOLUENE increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[43]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[44]
PMID28460551-Compound-3	DMA1FRM	Patented	PMID28460551-Compound-3 decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[21]
GW-501516	DMPL2KM	Discontinued in Phase 4	GW-501516 increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[26]
Tetramethylpyrazine	DMC0WNB	Discontinued in Phase 2	Tetramethylpyrazine increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[45]
NS398	DMINUWH	Terminated	NS398 decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[16]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[46]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[47]
Nickel chloride	DMI12Y8	Investigative	Nickel chloride increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[48]
Rapamycin Immunosuppressant Drug	DM678IB	Investigative	Rapamycin Immunosuppressant Drug increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[49]
Tributylstannanyl	DMHN7CB	Investigative	Tributylstannanyl increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[50]
Dibutyl phthalate	DMEDGKO	Investigative	Dibutyl phthalate decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[52]
Paraoxon	DMN4ZKC	Investigative	Paraoxon decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[53]
	DM9CEI5		decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[27]
27-hydroxycholesterol	DM2L6OZ	Investigative	27-hydroxycholesterol increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[54]
GW-3965	DMG60ET	Investigative	GW-3965 increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[55]
T0901317	DMZQVDI	Investigative	T0901317 increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[56]
Icosapentum	DMF1CM7	Investigative	Icosapentum decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[57]
24(S)-hydroxycholesterol	DMGMWA6	Investigative	24(S)-hydroxycholesterol increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[54]
2-chloro-5-nitro-N-phenylbenzamide	DMUGQIV	Investigative	2-chloro-5-nitro-N-phenylbenzamide decreases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[58]
24(S), 25-epoxycholesterol	DMW2KI5	Investigative	24(S), 25-epoxycholesterol increases the expression of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[59]

4 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Arachidonic acid	DMUOQZD	Investigative	Arachidonic acid increases the degradation of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[51]
Oleic acid	DM54O1Z	Investigative	Oleic acid increases the degradation of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[51]
Linoleic acid	DMDGPY9	Investigative	Linoleic acid increases the degradation of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[51]
Palmitoleic Acid	DM4W5X8	Investigative	Palmitoleic Acid increases the degradation of Phospholipid-transporting ATPase ABCA1 (ABCA1).	[51]

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