Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT0ISKQ4)

• DOT Name: Sulfotransferase 2A1 (SULT2A1)
• Synonyms: ST2A1; EC 2.8.2.2; Bile salt sulfotransferase; EC 2.8.2.14; Dehydroepiandrosterone sulfotransferase; DHEA-ST; DHEA-ST8; Hydroxysteroid Sulfotransferase; HST; ST2; SULT2A3
• Gene Name: SULT2A1
• UniProt ID: ST2A1_HUMAN
• PDB ID: 1EFH; 1J99; 1OV4; 2QP3; 2QP4; 3F3Y; 4IFB
• EC Number: 2.8.2.14; 2.8.2.2
• Pfam ID: PF00685
• Sequence:
  MSDDFLWFEGIAFPTMGFRSETLRKVRDEFVIRDEDVIILTYPKSGTNWLAEILCLMHSK
  GDAKWIQSVPIWERSPWVESEIGYTALSETESPRLFSSHLPIQLFPKSFFSSKAKVIYLM
  RNPRDVLVSGYFFWKNMKFIKKPKSWEEYFEWFCQGTVLYGSWFDHIHGWMPMREEKNFL
  LLSYEELKQDTGRTIEKICQFLGKTLEPEELNLILKNSSFQSMKENKMSNYSLLSVDYVV
  DKAQLLRKGVSGDWKNHFTVAQAEDFDKLFQEKMADLPRELFPWE
• Function: Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfonation of steroids and bile acids in the liver and adrenal glands. Mediates the sulfation of a wide range of steroids and sterols, including pregnenolone, androsterone, DHEA, bile acids, cholesterol and as well many xenobiotics that contain alcohol and phenol functional groups. Sulfonation increases the water solubility of most compounds, and therefore their renal excretion, but it can also result in bioactivation to form active metabolites. Plays an important role in maintening steroid and lipid homeostasis. Plays a key role in bile acid metabolism. In addition, catalyzes the metabolic activation of potent carcinogenic polycyclic arylmethanols.
• Tissue Specificity: Liver, adrenal and at lower level in the kidney. Is present in human fetus in higher level in the adrenal than the liver and the kidney.
• KEGG Pathway:
  Metabolism of xenobiotics by cytochrome P450 (hsa00980)
  Bile secretion (hsa04976)
  Chemical carcinogenesis - D. adducts (hsa05204)
• Reactome Pathway:
  PPARA activates gene expression (R-HSA-1989781)
  Paracetamol ADME (R-HSA-9753281)
  Cytosolic sulfonation of small molecules (R-HSA-156584)
• BioCyc Pathway: MetaCyc:HS02732-MONOMER

Molecular Interaction Atlas (MIA) of This DOT

This DOT Affected the Regulation of Drug Effects of 4 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Diethylstilbestrol	DMN3UXQ	Approved	Sulfotransferase 2A1 (SULT2A1) increases the metabolism of Diethylstilbestrol.	[29]
Ethinyl estradiol	DMODJ40	Approved	Sulfotransferase 2A1 (SULT2A1) increases the metabolism of Ethinyl estradiol.	[29]
Estrone	DM5T6US	Approved	Sulfotransferase 2A1 (SULT2A1) increases the metabolism of Estrone.	[29]
Mononitrophenol	DM4QO9G	Investigative	Sulfotransferase 2A1 (SULT2A1) increases the metabolism of Mononitrophenol.	[29]

This DOT Affected the Biotransformations of 4 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Ursodeoxycholic acid	DMCUT21	Approved	Sulfotransferase 2A1 (SULT2A1) increases the sulfation of Ursodeoxycholic acid.	[30]
Cholic acid	DM7OKQV	Approved	Sulfotransferase 2A1 (SULT2A1) increases the sulfation of Cholic acid.	[30]
	DM9CEI5		Sulfotransferase 2A1 (SULT2A1) increases the sulfation of .	[30]
BETULIN	DMGQRON	Investigative	Sulfotransferase 2A1 (SULT2A1) increases the sulfation of BETULIN.	[31]

34 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 Sulfotransferase 2A1 (SULT2A1).	[1]
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[2]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[3]
Acetaminophen	DMUIE76	Approved	Acetaminophen decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[4]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[5]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[2]
Arsenic	DMTL2Y1	Approved	Arsenic decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[6]
Quercetin	DM3NC4M	Approved	Quercetin decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[7]
Hydrogen peroxide	DM1NG5W	Approved	Hydrogen peroxide increases the expression of Sulfotransferase 2A1 (SULT2A1).	[8]
Triclosan	DMZUR4N	Approved	Triclosan decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[9]
Methotrexate	DM2TEOL	Approved	Methotrexate decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[10]
Isotretinoin	DM4QTBN	Approved	Isotretinoin increases the expression of Sulfotransferase 2A1 (SULT2A1).	[3]
Ethanol	DMDRQZU	Approved	Ethanol decreases the activity of Sulfotransferase 2A1 (SULT2A1).	[11]
Alitretinoin	DMME8LH	Approved	Alitretinoin decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[3]
Lindane	DMB8CNL	Approved	Lindane decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[12]
Nefazodone	DM4ZS8M	Approved	Nefazodone decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[13]
Chenodiol	DMQ8JIK	Approved	Chenodiol decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[14]
Atazanavir	DMSYRBX	Approved	Atazanavir decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[13]
Ciprofibrate	DMGC5DB	Approved	Ciprofibrate increases the expression of Sulfotransferase 2A1 (SULT2A1).	[15]
Urethane	DM7NSI0	Phase 4	Urethane decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[16]
Genistein	DM0JETC	Phase 2/3	Genistein increases the expression of Sulfotransferase 2A1 (SULT2A1).	[17]
Belinostat	DM6OC53	Phase 2	Belinostat decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[18]
Ibrolipim	DMOPWSX	Phase 2	Ibrolipim increases the expression of Sulfotransferase 2A1 (SULT2A1).	[19]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[20]
Leflunomide	DMR8ONJ	Phase 1 Trial	Leflunomide increases the expression of Sulfotransferase 2A1 (SULT2A1).	[21]
PMID26394986-Compound-22	DM43Z1G	Patented	PMID26394986-Compound-22 affects the activity of Sulfotransferase 2A1 (SULT2A1).	[23]
Antalarmin	DM2EKX5	Terminated	Antalarmin decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[24]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[25]
OXYQUINOLINE	DMZVS9Y	Investigative	OXYQUINOLINE increases the expression of Sulfotransferase 2A1 (SULT2A1).	[7]
Forskolin	DM6ITNG	Investigative	Forskolin decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[12]
all-trans-4-oxo-retinoic acid	DMM2R1N	Investigative	all-trans-4-oxo-retinoic acid decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[3]
Piceatannol	DMYOP45	Investigative	Piceatannol decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[26]
T0901317	DMZQVDI	Investigative	T0901317 increases the expression of Sulfotransferase 2A1 (SULT2A1).	[27]
astressin	DMSFLTK	Investigative	astressin decreases the expression of Sulfotransferase 2A1 (SULT2A1).	[24]

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 Sulfotransferase 2A1 (SULT2A1).	[22]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
adenosine-3'-5'-bisphosphate	DMSOVFD	Investigative	adenosine-3'-5'-bisphosphate affects the binding of Sulfotransferase 2A1 (SULT2A1).	[28]

References

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