Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT67HLNS)

• DOT Name: Taste receptor type 2 member 16 (TAS2R16)
• Synonyms: T2R16
• Gene Name: TAS2R16
• Related Disease:
  Alcohol dependence
  Alcohol use disorder
  Colon cancer
  Colon carcinoma
  Colorectal carcinoma
  Neoplasm
  Nicotine dependence
  Rectal carcinoma
  Neuroblastoma
  Colorectal adenoma
• UniProt ID: T2R16_HUMAN
• Pfam ID: PF05296
• Sequence:
  MIPIQLTVFFMIIYVLESLTIIVQSSLIVAVLGREWLQVRRLMPVDMILISLGISRFCLQ
  WASMLNNFCSYFNLNYVLCNLTITWEFFNILTFWLNSLLTVFYCIKVSSFTHHIFLWLRW
  RILRLFPWILLGSLMITCVTIIPSAIGNYIQIQLLTMEHLPRNSTVTDKLENFHQYQFQA
  HTVALVIPFILFLASTIFLMASLTKQIQHHSTGHCNPSMKARFTALRSLAVLFIVFTSYF
  LTILITIIGTLFDKRCWLWVWEAFVYAFILMHSTSLMLSSPTLKRILKGKC
• Function: Gustducin-coupled receptor implicated in the perception of bitter compounds in the oral cavity and the gastrointestinal tract. Signals through PLCB2 and the calcium-regulated cation channel TRPM5.
• Tissue Specificity: Expressed in a subset of gustducin-positive taste receptor cells of the tongue. Expressed in circumvallate papillae and testis .
• KEGG Pathway: Taste transduction (hsa04742)
• Reactome Pathway:
  Class C/3 (Metabotropic glutamate/pheromone receptors) (R-HSA-420499)
  Sensory perception of sweet, bitter, and umami (glutamate) taste (R-HSA-9717207)
  G alpha (i) signalling events (R-HSA-418594)

Molecular Interaction Atlas (MIA) of This DOT

10 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Alcohol dependence	DIS4ZSCO	Strong	Biomarker	[1]
Alcohol use disorder	DISMB65Y	Strong	Biomarker	[1]
Colon cancer	DISVC52G	Strong	Genetic Variation	[2]
Colon carcinoma	DISJYKUO	Strong	Genetic Variation	[2]
Colorectal carcinoma	DIS5PYL0	Strong	Genetic Variation	[2]
Neoplasm	DISZKGEW	Strong	Biomarker	[2]
Nicotine dependence	DISZD9W7	Strong	Biomarker	[3]
Rectal carcinoma	DIS8FRR7	Strong	Genetic Variation	[2]
Neuroblastoma	DISVZBI4	Disputed	Altered Expression	[4]
Colorectal adenoma	DISTSVHM	Limited	Genetic Variation	[5]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the methylation of Taste receptor type 2 member 16 (TAS2R16).	[6]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the methylation of Taste receptor type 2 member 16 (TAS2R16).	[8]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Salicin	DM1T2LS	Approved	Salicin increases the activity of Taste receptor type 2 member 16 (TAS2R16).	[7]

References

• [1] Functional variants in TAS2R38 and TAS2R16 influence alcohol consumption in high-risk families of African-American origin.Alcohol Clin Exp Res. 2007 Feb;31(2):209-15. doi: 10.1111/j.1530-0277.2006.00297.x.
• [2] Association between polymorphisms of TAS2R16 and susceptibility to colorectal cancer.BMC Gastroenterol. 2017 Sep 15;17(1):104. doi: 10.1186/s12876-017-0659-9.
• [3] A combinatorial approach to detecting gene-gene and gene-environment interactions in family studies.Am J Hum Genet. 2008 Oct;83(4):457-67. doi: 10.1016/j.ajhg.2008.09.001. Epub 2008 Oct 2.
• [4] Integrated olfaction, gustation and toxicity detection by a versatile bioengineered cell-based biomimetic sensor.Bioelectrochemistry. 2019 Aug;128:1-8. doi: 10.1016/j.bioelechem.2019.02.009. Epub 2019 Feb 21.
• [5] Variations in bitter-taste receptor genes, dietary intake, and colorectal adenoma risk.Nutr Cancer. 2013;65(7):982-90. doi: 10.1080/01635581.2013.807934. Epub 2013 Oct 1.
• [6] Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
• [7] Probenecid inhibits the human bitter taste receptor TAS2R16 and suppresses bitter perception of salicin. PLoS One. 2011;6(5):e20123.
• [8] Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.