Details of Drug Off-Target (DOT)

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

• DOT Name: Neuropeptide Y receptor type 5 (NPY5R)
• Synonyms: NPY5-R; NPY-Y5 receptor; NPYY5-R; Y5 receptor
• Gene Name: NPY5R
• UniProt ID: NPY5R_HUMAN
• Pfam ID: PF00001
• Sequence:
  MDLELDEYYNKTLATENNTAATRNSDFPVWDDYKSSVDDLQYFLIGLYTFVSLLGFMGNL
  LILMALMKKRNQKTTVNFLIGNLAFSDILVVLFCSPFTLTSVLLDQWMFGKVMCHIMPFL
  QCVSVLVSTLILISIAIVRYHMIKHPISNNLTANHGYFLIATVWTLGFAICSPLPVFHSL
  VELQETFGSALLSSRYLCVESWPSDSYRIAFTISLLLVQYILPLVCLTVSHTSVCRSISC
  GLSNKENRLEENEMINLTLHPSKKSGPQVKLSGSHKWSYSFIKKHRRRYSKKTACVLPAP
  ERPSQENHSRILPENFGSVRSQLSSSSKFIPGVPTCFEIKPEENSDVHELRVKRSVTRIK
  KRSRSVFYRLTILILVFAVSWMPLHLFHVVTDFNDNLISNRHFKLVYCICHLLGMMSCCL
  NPILYGFLNNGIKADLVSLIHCLHM
• Function: Receptor for neuropeptide Y and peptide YY. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity. Seems to be associated with food intake. Could be involved in feeding disorders.
• Tissue Specificity: Brain; hypothalamus.
• KEGG Pathway: Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Peptide ligand-binding receptors (R-HSA-375276)

Molecular Interaction Atlas (MIA) of This DOT

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the expression of Neuropeptide Y receptor type 5 (NPY5R).	[1]
Tretinoin	DM49DUI	Approved	Tretinoin increases the expression of Neuropeptide Y receptor type 5 (NPY5R).	[2]
Estradiol	DMUNTE3	Approved	Estradiol increases the expression of Neuropeptide Y receptor type 5 (NPY5R).	[3]
Folic acid	DMEMBJC	Approved	Folic acid decreases the expression of Neuropeptide Y receptor type 5 (NPY5R).	[4]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A decreases the expression of Neuropeptide Y receptor type 5 (NPY5R).	[1]
QUERCITRIN	DM1DH96	Investigative	QUERCITRIN increases the expression of Neuropeptide Y receptor type 5 (NPY5R).	[6]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene affects the methylation of Neuropeptide Y receptor type 5 (NPY5R).	[5]

References

• [1] From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
• [2] Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
• [3] Long-term estrogen exposure promotes carcinogen bioactivation, induces persistent changes in gene expression, and enhances the tumorigenicity of MCF-7 human breast cancer cells. Toxicol Appl Pharmacol. 2009 Nov 1;240(3):355-66.
• [4] Folic acid supplementation dysregulates gene expression in lymphoblastoid cells--implications in nutrition. Biochem Biophys Res Commun. 2011 Sep 9;412(4):688-92. doi: 10.1016/j.bbrc.2011.08.027. Epub 2011 Aug 16.
• [5] 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.
• [6] Molecular mechanisms of quercitrin-induced apoptosis in non-small cell lung cancer. Arch Med Res. 2014 Aug;45(6):445-54.