Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTUY8CGM)

DOT Name	Trace amine-associated receptor 1 (TAAR1)
Synonyms	TaR-1; Trace amine receptor 1
Gene Name	TAAR1
UniProt ID	TAAR1_HUMAN
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
PDB ID	8JLN; 8JLO; 8JLP; 8JLQ; 8JLR; 8JSO; 8W87; 8W88; 8W89; 8W8A
Pfam ID	PF00001
Sequence	MMPFCHNIINISCVKNNWSNDVRASLYSLMVLIILTTLVGNLIVIVSISHFKQLHTPTNW LIHSMATVDFLLGCLVMPYSMVRSAEHCWYFGEVFCKIHTSTDIMLSSASIFHLSFISID RYYAVCDPLRYKAKMNILVICVMIFISWSVPAVFAFGMIFLELNFKGAEEIYYKHVHCRG GCSVFFSKISGVLTFMTSFYIPGSIMLCVYYRIYLIAKEQARLISDANQKLQIGLEMKNG ISQSKERKAVKTLGIVMGVFLICWCPFFICTVMDPFLHYIIPPTLNDVLIWFGYLNSTFN PMVYAFFYPWFRKALKMMLFGKIFQKDSSRCKLFLELSS
Function	Receptor for trace amines, including beta-phenylethylamine (b-PEA), p-tyramine (p-TYR), octopamine and tryptamine, with highest affinity for b-PEA and p-TYR. Unresponsive to classical biogenic amines, such as epinephrine and histamine and only partially activated by dopamine and serotonin. Trace amines are biogenic amines present in very low levels in mammalian tissues. Although some trace amines have clearly defined roles as neurotransmitters in invertebrates, the extent to which they function as true neurotransmitters in vertebrates has remained speculative. Trace amines are likely to be involved in a variety of physiological functions that have yet to be fully understood. The signal transduced by this receptor is mediated by the G(s)-class of G-proteins which activate adenylate cyclase.
Tissue Specificity	Detected in low levels in discrete regions within the central nervous system and in several peripheral tissues. Moderately expressed in stomach. Low levels in amygdala, kidney, and lung, and small intestine. Trace amounts in cerebellum, dorsal root ganglia, hippocampus, hypothalamus, liver, medulla, pancreas, pituitary, pontine reticular formation, prostate, skeletal muscle and spleen.
KEGG Pathway	Neuroactive ligand-receptor interaction (hsa04080 )
Reactome Pathway	G alpha (s) signalling events (R-HSA-418555 ) Amine ligand-binding receptors (R-HSA-375280 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA)

MIA Detail

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

Drug Name	Drug ID	Highest Status	Interaction	REF
TRYPTAMINE	DMAFPHB	Phase 3	TRYPTAMINE increases the activity of Trace amine-associated receptor 1 (TAAR1).	[1]
Octopamine	DMLQVTJ	Discontinued in Phase 2a	Octopamine increases the activity of Trace amine-associated receptor 1 (TAAR1).	[1]
Phenethylamine	DMX0G4F	Investigative	Phenethylamine increases the activity of Trace amine-associated receptor 1 (TAAR1).	[1]
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References

1	Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands. Biochem J. 2009 Oct 23;424(1):39-45. doi: 10.1042/BJ20090998.