Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Orphan nuclear receptor NR1I3 (NR1I3)
• Synonyms: Orphan nuclear receptor MB67; Orphan nuclear receptor CAR; Nuclear receptor subfamily 1 group I member 3; Nuclear receptor CAR; Constitutive androstane receptor; Constitutive active response; Constitutive activator of retinoid response; CAR
• Gene Name: NR1I3
• DTT Type: Successful target; [1]
• BioChemical Class: Nuclear hormone receptor
• UniProt ID: NR1I3_HUMAN
• TTD ID: T69506
• Sequence:
  MASREDELRNCVVCGDQATGYHFNALTCEGCKGFFRRTVSKSIGPTCPFAGSCEVSKTQR
  RHCPACRLQKCLDAGMRKDMILSAEALALRRAKQAQRRAQQTPVQLSKEQEELIRTLLGA
  HTRHMGTMFEQFVQFRPPAHLFIHHQPLPTLAPVLPLVTHFADINTFMVLQVIKFTKDLP
  VFRSLPIEDQISLLKGAAVEICHIVLNTTFCLQTQNFLCGPLRYTIEDGARVSPTVGFQV
  EFLELLFHFHGTLRKLQLQEPEYVLLAAMALFSPDRPGVTQRDEIDQLQEEMALTLQSYI
  KGQQRRPRDRFLYAKLLGLLAELRSINEAYGYQIQHIQGLSAMMPLLQEICS
• Function: Transactivates both the phenobarbital responsive element module of the human CYP2B6 gene and the CYP3A4 xenobiotic response element. Binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor beta 2 and alcohol dehydrogenase 3 genes.
• KEGG Pathway: Chemical carcinogenesis - receptor activation (hsa05207)
• Reactome Pathway: Nuclear Receptor transcription pathway (R-HSA-383280)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Meclizine	DMS7T13	Dizziness	MB48	Approved	[1]

5 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(5BETA)-PREGNANE-3,20-DIONE	DMVQ6RN	Discovery agent	N.A.	Investigative	[2]
androstanol	DMPXF5I	Discovery agent	N.A.	Investigative	[3]
androstenol	DM7RXQ6	Discovery agent	N.A.	Investigative	[3]
CITCO	DM0N634	Discovery agent	N.A.	Investigative	[4]
TCPOBOP	DMKVF5Q	Discovery agent	N.A.	Investigative	[5]

References

• [1] Synthetic drugs and natural products as modulators of constitutive androstane receptor (CAR) and pregnane X receptor (PXR). Drug Metab Rev. 2006;38(1-2):51-73.
• [2] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [3] Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta. Nature. 1998 Oct 8;395(6702):612-5.
• [4] Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes. J Biol Chem. 2003 May 9;278(19):17277-83.
• [5] The nuclear receptor CAR is a regulator of thyroid hormone metabolism during caloric restriction. J Biol Chem. 2004 May 7;279(19):19832-8.