Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTTMOJ8U)

• DOT Name: Mas-related G-protein coupled receptor member D (MRGPRD)
• Synonyms: Beta-alanine receptor; G-protein coupled receptor TGR7
• Gene Name: MRGPRD
• Related Disease:
  Dilated cardiomyopathy
  Lung cancer
  Neoplasm
  Neuralgia
  Non-small-cell lung cancer
• UniProt ID: MRGRD_HUMAN
• PDB ID: 7Y12; 7Y13; 7Y14; 7Y15
• Pfam ID: PF00001
• Sequence:
  MNQTLNSSGTVESALNYSRGSTVHTAYLVLSSLAMFTCLCGMAGNSMVIWLLGFRMHRNP
  FCIYILNLAAADLLFLFSMASTLSLETQPLVNTTDKVHELMKRLMYFAYTVGLSLLTAIS
  TQRCLSVLFPIWFKCHRPRHLSAWVCGLLWTLCLLMNGLTSSFCSKFLKFNEDRCFRVDM
  VQAALIMGVLTPVMTLSSLTLFVWVRRSSQQWRRQPTRLFVVVLASVLVFLICSLPLSIY
  WFVLYWLSLPPEMQVLCFSLSRLSSSVSSSANPVIYFLVGSRRSHRLPTRSLGTVLQQAL
  REEPELEGGETPTVGTNEMGA
• Function: May regulate nociceptor function and/or development, including the sensation or modulation of pain. Functions as a specific membrane receptor for beta-alanine. Beta-alanine at micromolar doses specifically evoked Ca(2+) influx in cells expressing the receptor. Beta-alanine decreases forskolin-stimulated cAMP production in cells expressing the receptor, suggesting that the receptor couples with G-protein G(q) and G(i).
• KEGG Pathway: Renin-angiotensin system (hsa04614)

Molecular Interaction Atlas (MIA) of This DOT

5 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Dilated cardiomyopathy	DISX608J	Strong	Biomarker	[1]
Lung cancer	DISCM4YA	Strong	Altered Expression	[2]
Neoplasm	DISZKGEW	Strong	Altered Expression	[2]
Neuralgia	DISWO58J	Strong	Biomarker	[3]
Non-small-cell lung cancer	DIS5Y6R9	Strong	Altered Expression	[2]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the expression of Mas-related G-protein coupled receptor member D (MRGPRD).	[4]

References

• [1] Genetic deletion of the alamandine receptor MRGD leads to dilated cardiomyopathy in mice.Am J Physiol Heart Circ Physiol. 2019 Jan 1;316(1):H123-H133. doi: 10.1152/ajpheart.00075.2018. Epub 2018 Oct 19.
• [2] Expression and clinical contribution of MRGD mRNA in non-small cell lung cancers.J BUON. 2015 Jul-Aug;20(4):1101-6.
• [3] Identification of a G protein-coupled receptor specifically responsive to beta-alanine.J Biol Chem. 2004 May 28;279(22):23559-64. doi: 10.1074/jbc.M314240200. Epub 2004 Mar 22.
• [4] Benzo[a]pyrene-induced changes in microRNA-mRNA networks. Chem Res Toxicol. 2012 Apr 16;25(4):838-49.