Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT5BG6MK)

DOT Name ATP-binding cassette sub-family G member 1 (ABCG1)
Synonyms EC 7.6.2.-; ATP-binding cassette transporter 8; White protein homolog
Gene Name ABCG1
UniProt ID
ABCG1_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
7FDV; 7OZ1; 7R8C; 7R8D; 7R8E
EC Number
7.6.2.-
Pfam ID
PF01061 ; PF19055 ; PF00005
Sequence
MACLMAAFSVGTAMNASSYSAEMTEPKSVCVSVDEVVSSNMEATETDLLNGHLKKVDNNL
TEAQRFSSLPRRAAVNIEFRDLSYSVPEGPWWRKKGYKTLLKGISGKFNSGELVAIMGPS
GAGKSTLMNILAGYRETGMKGAVLINGLPRDLRCFRKVSCYIMQDDMLLPHLTVQEAMMV
SAHLKLQEKDEGRREMVKEILTALGLLSCANTRTGSLSGGQRKRLAIALELVNNPPVMFF
DEPTSGLDSASCFQVVSLMKGLAQGGRSIICTIHQPSAKLFELFDQLYVLSQGQCVYRGK
VCNLVPYLRDLGLNCPTYHNPADFVMEVASGEYGDQNSRLVRAVREGMCDSDHKRDLGGD
AEVNPFLWHRPSEEVKQTKRLKGLRKDSSSMEGCHSFSASCLTQFCILFKRTFLSIMRDS
VLTHLRITSHIGIGLLIGLLYLGIGNEAKKVLSNSGFLFFSMLFLMFAALMPTVLTFPLE
MGVFLREHLNYWYSLKAYYLAKTMADVPFQIMFPVAYCSIVYWMTSQPSDAVRFVLFAAL
GTMTSLVAQSLGLLIGAASTSLQVATFVGPVTAIPVLLFSGFFVSFDTIPTYLQWMSYIS
YVRYGFEGVILSIYGLDREDLHCDIDETCHFQKSEAILRELDVENAKLYLDFIVLGIFFI
SLRLIAYFVLRYKIRAER
Function
Catalyzes the efflux of phospholipids such as sphingomyelin, cholesterol and its oxygenated derivatives like 7beta-hydroxycholesterol and this transport is coupled to hydrolysis of ATP. The lipid efflux is ALB-dependent. Is an active component of the macrophage lipid export complex. Could also be involved in intracellular lipid transport processes. The role in cellular lipid homeostasis may not be limited to macrophages. Prevents cell death by transporting cytotoxic 7beta-hydroxycholesterol.
Tissue Specificity Expressed in several tissues. Expressed in macrophages; expression is increased in macrophages from patients with Tangier disease.
KEGG Pathway
ABC transporters (hsa02010 )
Lipid and atherosclerosis (hsa05417 )
Reactome Pathway
HDL remodeling (R-HSA-8964058 )
NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux (R-HSA-9029569 )
ABC transporters in lipid homeostasis (R-HSA-1369062 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 1 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Docetaxel DMDI269 Approved ATP-binding cassette sub-family G member 1 (ABCG1) affects the response to substance of Docetaxel. [37]
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45 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [1]
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [2]
Tretinoin DM49DUI Approved Tretinoin increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [3]
Acetaminophen DMUIE76 Approved Acetaminophen increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [4]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [5]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [6]
Triclosan DMZUR4N Approved Triclosan increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [7]
Decitabine DMQL8XJ Approved Decitabine affects the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [8]
Marinol DM70IK5 Approved Marinol decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [9]
Progesterone DMUY35B Approved Progesterone decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [10]
Rosiglitazone DMILWZR Approved Rosiglitazone increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [11]
Ethanol DMDRQZU Approved Ethanol decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [12]
Nicotine DMWX5CO Approved Nicotine decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [13]
Clozapine DMFC71L Approved Clozapine increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [14]
Amphotericin B DMTAJQE Approved Amphotericin B decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [15]
Cidofovir DMA13GD Approved Cidofovir decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [5]
Simvastatin DM30SGU Approved Simvastatin decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [16]
Obeticholic acid DM3Q1SM Approved Obeticholic acid decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [17]
Rifampicin DM5DSFZ Approved Rifampicin increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [18]
Ifosfamide DMCT3I8 Approved Ifosfamide decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [5]
Clodronate DM9Y6X7 Approved Clodronate decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [5]
Alitretinoin DMME8LH Approved Alitretinoin increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [19]
Ibuprofen DM8VCBE Approved Ibuprofen increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [5]
Lindane DMB8CNL Approved Lindane increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [20]
SNDX-275 DMH7W9X Phase 3 SNDX-275 increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [21]
Resveratrol DM3RWXL Phase 3 Resveratrol increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [22]
Epigallocatechin gallate DMCGWBJ Phase 3 Epigallocatechin gallate decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [23]
Curcumin DMQPH29 Phase 3 Curcumin increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [24]
Telmisartan DMS3GX2 Phase 3 Trial Telmisartan increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [25]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [26]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [27]
Trichostatin A DM9C8NX Investigative Trichostatin A decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [29]
3R14S-OCHRATOXIN A DM2KEW6 Investigative 3R14S-OCHRATOXIN A decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [20]
Nickel chloride DMI12Y8 Investigative Nickel chloride increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [30]
Hexadecanoic acid DMWUXDZ Investigative Hexadecanoic acid increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [19]
Tributylstannanyl DMHN7CB Investigative Tributylstannanyl increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [31]
Arachidonic acid DMUOQZD Investigative Arachidonic acid decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [19]
Dibutyl phthalate DMEDGKO Investigative Dibutyl phthalate decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [32]
Oleic acid DM54O1Z Investigative Oleic acid decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [19]
27-hydroxycholesterol DM2L6OZ Investigative 27-hydroxycholesterol increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [33]
GW-3965 DMG60ET Investigative GW-3965 increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [34]
Linoleic acid DMDGPY9 Investigative Linoleic acid decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [19]
T0901317 DMZQVDI Investigative T0901317 increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [35]
Icosapentum DMF1CM7 Investigative Icosapentum decreases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [19]
24(S)-hydroxycholesterol DMGMWA6 Investigative 24(S)-hydroxycholesterol increases the expression of ATP-binding cassette sub-family G member 1 (ABCG1). [36]
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⏷ Show the Full List of 45 Drug(s)
1 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the methylation of ATP-binding cassette sub-family G member 1 (ABCG1). [28]
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References

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19 Unsaturated fatty acids suppress the expression of the ATP-binding cassette transporter G1 (ABCG1) and ABCA1 genes via an LXR/RXR responsive element. Atherosclerosis. 2007 Mar;191(1):11-21. doi: 10.1016/j.atherosclerosis.2006.04.018. Epub 2006 May 30.
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