Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT79TKF)

• DTT Name: HepG2 glucose transporter (SLC2A1)
• Synonyms: Solute carrier family 2, facilitated glucose transporter member 1; HepG2 glucosetransporter; Glucose transporter type 1, erythrocyte/brain; GLUT1; GLUT-1
• Gene Name: SLC2A1
• DTT Type: Preclinical target; [1]
• BioChemical Class: Major facilitator
• UniProt ID: GTR1_HUMAN
• TTD ID: T89458
• Sequence:
  MEPSSKKLTGRLMLAVGGAVLGSLQFGYNTGVINAPQKVIEEFYNQTWVHRYGESILPTT
  LTTLWSLSVAIFSVGGMIGSFSVGLFVNRFGRRNSMLMMNLLAFVSAVLMGFSKLGKSFE
  MLILGRFIIGVYCGLTTGFVPMYVGEVSPTALRGALGTLHQLGIVVGILIAQVFGLDSIM
  GNKDLWPLLLSIIFIPALLQCIVLPFCPESPRFLLINRNEENRAKSVLKKLRGTADVTHD
  LQEMKEESRQMMREKKVTILELFRSPAYRQPILIAVVLQLSQQLSGINAVFYYSTSIFEK
  AGVQQPVYATIGSGIVNTAFTVVSLFVVERAGRRTLHLIGLAGMAGCAILMTIALALLEQ
  LPWMSYLSIVAIFGFVAFFEVGPGPIPWFIVAELFSQGPRPAAIAVAGFSNWTSNFIVGM
  CFQYVEQLCGPYVFIIFTVLLVLFFIFTYFKVPETKGRTFDEIASGFRQGGASQSDKTPE
  ELFHPLGADSQV
• Function: Facilitative glucose transporter. This isoform may be 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.
• KEGG Pathway:
  HIF-1 signaling pathway (hsa04066)
  Insulin secretion (hsa04911)
  Thyroid hormone signaling pathway (hsa04919)
  Adipocytokine signaling pathway (hsa04920)
  Glucagon signaling pathway (hsa04922)
  Insulin resistance (hsa04931)
  Bile secretion (hsa04976)
  Human T-cell leukemia virus 1 infection (hsa05166)
  Pathways in cancer (hsa05200)
  Renal 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-MON

Molecular Interaction Atlas (MIA) of This DTT

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
WZB-117	DMKE5QH	Skin fibrosis	EM0Z	Preclinical	[2]

The Drug Transporter (DTP) Role of This DTT

• DTT DTP Name: Glucose transporter type 1, erythrocyte/brain (SLC2A1) DTP Info
• Gene Name: SLC2A1

2 Approved Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-deoxyglucose	DMIAHVU	Solid tumour/cancer	2A00-2F9Z	Approved	[3]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[4]

3 Investigative Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Arsenite	DMBCO4Q	Discovery agent	N.A.	Investigative	[5]
D-glucose	DMMG2TO	Discovery agent	N.A.	Investigative	[6]
dehydroascorbic acid	DMKYQO4	Discovery agent	N.A.	Investigative	[7]

References

• [1] GLUT1 messenger RNA and protein induction relates to the malignant transformation of cervical cancer. Am J Clin Pathol. 2003 Nov;120(5):691-8.
• [2] Quercetin inhibits glucose transport by binding to an exofacial site on GLUT1. Biochimie. 2018 Aug;151:107-114.
• [3] Glutamine 161 of Glut1 glucose transporter is critical for transport activity and exofacial ligand binding. J Biol Chem. 1994 Aug 12;269(32):20533-8.
• [4] Oral Bioavailability and Disposition of Phytochemicals
• [5] Mammalian glucose permease GLUT1 facilitates transport of arsenic trioxide and methylarsonous acid. Biochem Biophys Res Commun. 2006 Dec 15;351(2):424-30.
• [6] The SLC2 (GLUT) family of membrane transporters. Mol Aspects Med. 2013 Apr-Jun;34(2-3):121-38.
• [7] Glucose transporter isoforms GLUT1 and GLUT3 transport dehydroascorbic acid. J Biol Chem. 1997 Jul 25;272(30):18982-9.