Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTA675TJ)

DOT Name Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1)
Synonyms Glucose transporter type 1, erythrocyte/brain; GLUT-1; HepG2 glucose transporter
Gene Name SLC2A1
Related Disease
Childhood onset GLUT1 deficiency syndrome 2 ( )
Encephalopathy due to GLUT1 deficiency ( )
GLUT1 deficiency syndrome ( )
Dystonia 9 ( )
Epilepsy, idiopathic generalized, susceptibility to, 12 ( )
Absence seizure ( )
Hereditary cryohydrocytosis with reduced stomatin ( )
Myoclonic-astatic epilepsy ( )
UniProt ID
GTR1_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
4PYP; 5EQG; 5EQH; 5EQI; 6THA
Pfam ID
PF00083
Sequence
MEPSSKKLTGRLMLAVGGAVLGSLQFGYNTGVINAPQKVIEEFYNQTWVHRYGESILPTT
LTTLWSLSVAIFSVGGMIGSFSVGLFVNRFGRRNSMLMMNLLAFVSAVLMGFSKLGKSFE
MLILGRFIIGVYCGLTTGFVPMYVGEVSPTALRGALGTLHQLGIVVGILIAQVFGLDSIM
GNKDLWPLLLSIIFIPALLQCIVLPFCPESPRFLLINRNEENRAKSVLKKLRGTADVTHD
LQEMKEESRQMMREKKVTILELFRSPAYRQPILIAVVLQLSQQLSGINAVFYYSTSIFEK
AGVQQPVYATIGSGIVNTAFTVVSLFVVERAGRRTLHLIGLAGMAGCAILMTIALALLEQ
LPWMSYLSIVAIFGFVAFFEVGPGPIPWFIVAELFSQGPRPAAIAVAGFSNWTSNFIVGM
CFQYVEQLCGPYVFIIFTVLLVLFFIFTYFKVPETKGRTFDEIASGFRQGGASQSDKTPE
ELFHPLGADSQV
Function
Facilitative glucose transporter, which is responsible for constitutive or basal glucose uptake. Has a very broad substrate specificity; can transport a wide range of aldoses including both pentoses and hexoses. Most important energy carrier of the brain: present at the blood-brain barrier and assures the energy-independent, facilitative transport of glucose into the brain. In association with BSG and NXNL1, promotes retinal cone survival by increasing glucose uptake into photoreceptors. Required for mesendoderm differentiation.
Tissue Specificity Detected in erythrocytes (at protein level). Expressed at variable levels in many human tissues.
KEGG Pathway
HIF-1 sig.ling pathway (hsa04066 )
Efferocytosis (hsa04148 )
Insulin secretion (hsa04911 )
Thyroid hormone sig.ling pathway (hsa04919 )
Adipocytokine sig.ling pathway (hsa04920 )
Glucagon sig.ling pathway (hsa04922 )
Insulin resistance (hsa04931 )
Bile secretion (hsa04976 )
Human T-cell leukemia virus 1 infection (hsa05166 )
Pathways in cancer (hsa05200 )
Re.l cell carcinoma (hsa05211 )
Central carbon metabolism in cancer (hsa05230 )
Diabetic cardiomyopathy (hsa05415 )
Reactome Pathway
Vitamin C (ascorbate) metabolism (R-HSA-196836 )
Regulation of insulin secretion (R-HSA-422356 )
Defective SLC2A1 causes GLUT1 deficiency syndrome 1 (GLUT1DS1) (R-HSA-5619043 )
Lactose synthesis (R-HSA-5653890 )
Cellular hexose transport (R-HSA-189200 )
BioCyc Pathway
MetaCyc:ENSG00000117394-MONOMER

Molecular Interaction Atlas (MIA) of This DOT

8 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Childhood onset GLUT1 deficiency syndrome 2 DISXPRXM Definitive Autosomal dominant [1]
Encephalopathy due to GLUT1 deficiency DISFX0JQ Definitive Autosomal dominant [2]
GLUT1 deficiency syndrome DIS8OXEB Definitive Autosomal dominant [3]
Dystonia 9 DIS0KL38 Strong Autosomal dominant [4]
Epilepsy, idiopathic generalized, susceptibility to, 12 DIS90R1X Strong Autosomal dominant [5]
Absence seizure DIS4709R Supportive Autosomal dominant [6]
Hereditary cryohydrocytosis with reduced stomatin DISYP8Y8 Supportive Autosomal dominant [7]
Myoclonic-astatic epilepsy DISTAVMU Supportive Unknown [8]
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⏷ Show the Full List of 8 Disease(s)
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Regulation of Drug Effects of 2 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
2-deoxyglucose DMIAHVU Approved Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1) increases the uptake of 2-deoxyglucose. [76]
Dehydroascorbic acid DMKYQO4 Investigative Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1) decreases the transport of Dehydroascorbic acid. [79]
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This DOT Affected the Drug Response of 3 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Dacarbazine DMNPZL4 Approved Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1) decreases the response to substance of Dacarbazine. [77]
Captopril DM458UM Approved Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1) increases the Adverse drug reaction ADR of Captopril. [78]
Apaziquone DMVY0BU Phase 3 Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1) decreases the response to substance of Apaziquone. [77]
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80 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [9]
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [10]
Tretinoin DM49DUI Approved Tretinoin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [11]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [12]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate affects the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [13]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [14]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [15]
Ivermectin DMDBX5F Approved Ivermectin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [16]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [17]
Temozolomide DMKECZD Approved Temozolomide increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [18]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [19]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [20]
Vorinostat DMWMPD4 Approved Vorinostat decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [21]
Triclosan DMZUR4N Approved Triclosan increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [22]
Marinol DM70IK5 Approved Marinol decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [23]
Phenobarbital DMXZOCG Approved Phenobarbital decreases the activity of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [24]
Progesterone DMUY35B Approved Progesterone increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [25]
Menadione DMSJDTY Approved Menadione affects the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [26]
Fluorouracil DMUM7HZ Approved Fluorouracil decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [27]
Niclosamide DMJAGXQ Approved Niclosamide decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [28]
Cannabidiol DM0659E Approved Cannabidiol decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [29]
Troglitazone DM3VFPD Approved Troglitazone decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [30]
Diethylstilbestrol DMN3UXQ Approved Diethylstilbestrol decreases the activity of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [31]
Rosiglitazone DMILWZR Approved Rosiglitazone decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [32]
Cytarabine DMZD5QR Approved Cytarabine decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [33]
Cidofovir DMA13GD Approved Cidofovir increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [34]
Zidovudine DM4KI7O Approved Zidovudine decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [35]
Ifosfamide DMCT3I8 Approved Ifosfamide increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [34]
Ibuprofen DM8VCBE Approved Ibuprofen increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [34]
Benzatropine DMF7EXL Approved Benzatropine decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [29]
Liothyronine DM6IR3P Approved Liothyronine increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [36]
Imatinib DM7RJXL Approved Imatinib decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [37]
Propofol DMB4OLE Approved Propofol decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [39]
Sevoflurane DMC9O43 Approved Sevoflurane increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [39]
Ciprofloxacin XR DM2NLS9 Approved Ciprofloxacin XR decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [40]
Mebendazole DMO14SG Approved Mebendazole decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [41]
Aluminium DM6ECN9 Approved Aluminium increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [42]
Ofloxacin DM0VQN3 Approved Ofloxacin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [40]
Pentobarbital DMFNH7L Approved Pentobarbital decreases the activity of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [24]
Glycine DMIOZ29 Approved Glycine decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [43]
Cyclofenil DMT5RMB Approved Cyclofenil decreases the activity of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [31]
Dihydrotestosterone DM3S8XC Phase 4 Dihydrotestosterone increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [44]
Curcumin DMQPH29 Phase 3 Curcumin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [46]
Coprexa DMA0WEK Phase 3 Coprexa decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [47]
Acadesine DM1RMF5 Phase 3 Acadesine increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [48]
FG-4592 DM4XSQ2 Phase 3 FG-4592 increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [49]
Genistein DM0JETC Phase 2/3 Genistein decreases the activity of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [31]
Amiodarone DMUTEX3 Phase 2/3 Trial Amiodarone decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [50]
GDC0941 DM1YAK6 Phase 2 GDC0941 decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [51]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [53]
Leflunomide DMR8ONJ Phase 1 Trial Leflunomide increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [54]
LY294002 DMY1AFS Phase 1 LY294002 decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [55]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [56]
PMID26394986-Compound-22 DM43Z1G Patented PMID26394986-Compound-22 increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [58]
MG-132 DMKA2YS Preclinical MG-132 increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [59]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [60]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [61]
Formaldehyde DM7Q6M0 Investigative Formaldehyde increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [62]
chloropicrin DMSGBQA Investigative chloropicrin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [63]
Deguelin DMXT7WG Investigative Deguelin increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [64]
3R14S-OCHRATOXIN A DM2KEW6 Investigative 3R14S-OCHRATOXIN A increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [65]
Glyphosate DM0AFY7 Investigative Glyphosate increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [43]
Nickel chloride DMI12Y8 Investigative Nickel chloride increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [49]
D-glucose DMMG2TO Investigative D-glucose increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [48]
Phencyclidine DMQBEYX Investigative Phencyclidine increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [66]
Okadaic acid DM47CO1 Investigative Okadaic acid increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [67]
CH-223191 DMMJZYC Investigative CH-223191 increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [68]
PP-242 DM2348V Investigative PP-242 decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [69]
Kaempferol DMHEMUB Investigative Kaempferol decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [70]
Daidzein DMRFTJX Investigative Daidzein decreases the activity of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [31]
Apigenin DMI3491 Investigative Apigenin decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [71]
Myricetin DMTV4L0 Investigative Myricetin decreases the activity of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [31]
Protoporphyrin IX DMWYE7A Investigative Protoporphyrin IX decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [72]
Alpha-naphthoflavone DMELOIQ Investigative Alpha-naphthoflavone increases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [68]
DZNep DM0JXBK Investigative DZNep decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [73]
Phloretin DMYA50U Investigative Phloretin decreases the activity of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [31]
GW-788388 DMIBUW5 Investigative GW-788388 decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [50]
EPZ015666 DM3INX7 Investigative EPZ015666 decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [74]
NSC-94258 DM6VY3P Investigative NSC-94258 decreases the activity of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [31]
KAEMPFERIDE DMUWA2G Investigative KAEMPFERIDE decreases the expression of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [75]
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⏷ Show the Full List of 80 Drug(s)
3 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
Adenosine triphosphate DM79F6G Approved Adenosine triphosphate decreases the stability of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [38]
Resveratrol DM3RWXL Phase 3 Resveratrol affects the binding of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [45]
Preverex DMZT8FS Phase 2 Preverex affects the folding of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [52]
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1 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
PMID28870136-Compound-52 DMFDERP Patented PMID28870136-Compound-52 decreases the phosphorylation of Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1). [57]
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References

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2 Defective glucose transport across the blood-brain barrier as a cause of persistent hypoglycorrhachia, seizures, and developmental delay. N Engl J Med. 1991 Sep 5;325(10):703-9. doi: 10.1056/NEJM199109053251006.
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40 Disturbance of cellular glucose transport by two prevalently used fluoroquinolone antibiotics ciprofloxacin and levofloxacin involves glucose transporter type 1. Toxicol Lett. 2009 Jan 30;184(2):81-4. doi: 10.1016/j.toxlet.2008.10.017. Epub 2008 Oct 28.
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44 LSD1 activates a lethal prostate cancer gene network independently of its demethylase function. Proc Natl Acad Sci U S A. 2018 May 1;115(18):E4179-E4188.
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