Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTOPAY7)

• DTT Name: Galanin receptor (GAL-R)
• Synonyms: GALR; GALNR; GAL-R
• Gene Name: GALR1
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: GALR1_HUMAN ; GALR2_HUMAN ; GALR3_HUMAN
• TTD ID: T98494
• Sequence:
  MELAVGNLSEGNASWPEPPAPEPGPLFGIGVENFVTLVVFGLIFALGVLGNSLVITVLAR
  SKPGKPRSTTNLFILNLSIADLAYLLFCIPFQATVYALPTWVLGAFICKFIHYFFTVSML
  VSIFTLAAMSVDRYVAIVHSRRSSSLRVSRNALLGVGCIWALSIAMASPVAYHQGLFHPR
  ASNQTFCWEQWPDPRHKKAYVVCTFVFGYLLPLLLICFCYAKVLNHLHKKLKNMSKKSEA
  SKKKTAQTVLVVVVVFGISWLPHHIIHLWAEFGVFPLTPASFLFRITAHCLAYSNSSVNP
  IIYAFLSENFRKAYKQVFKCHIRKDSHLSDTKESKSRIDTPPSTNCTHV
• Function: Receptor for the hormone galanin. Receptor for the hormone spexin-1.
• 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 DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
HT-2157	DM7C1AJ	Cognitive impairment	6D71	Phase 1/2	[1]

9 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(E)-3-(2,3-dichlorophenylimino)indolin-2-one	DM1LG27	Discovery agent	N.A.	Investigative	[2]
(E)-3-(4-chlorophenylimino)indolin-2-one	DMPOYK2	Discovery agent	N.A.	Investigative	[2]
2,3-dihydro-1,4-dithiin-1,1,4,4-tetroxide	DMJB7W1	Discovery agent	N.A.	Investigative	[3]
CYM2503	DM5NFEA	Discovery agent	N.A.	Investigative	[4]
dithiipin-1,1,4,4-tetroxide analogue 7	DMK0VFS	Discovery agent	N.A.	Investigative	[3]
galmic	DML9DH8	Discovery agent	N.A.	Investigative	[5]
GalR3ant	DMI7RPT	Discovery agent	N.A.	Investigative	[6]
Sch 202596	DMRC4LE	Discovery agent	N.A.	Investigative	[7]
SNAP 398299	DMS1AFL	Discovery agent	N.A.	Investigative	[1]

References

• [1] Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299. Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17489-94.
• [2] 3-arylimino-2-indolones are potent and selective galanin GAL3 receptor antagonists. J Med Chem. 2006 Jun 29;49(13):3757-8.
• [3] 2,3-Dihydro-dithiin and -dithiepine-1,1,4,4-tetroxides: small molecule non-peptide antagonists of the human galanin hGAL-1 receptor. Bioorg Med Chem. 2000 Jun;8(6):1383-91.
• [4] GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15229-34.
• [5] Galmic, a nonpeptide galanin receptor agonist, affects behaviors in seizure, pain, and forced-swim tests. Proc Natl Acad Sci U S A. 2004 Jul 13;101(28):10470-5.
• [6] Galanin (2-11) binds to GalR3 in transfected cell lines: limitations for pharmacological definition of receptor subtypes. Neuropeptides. 2005 Jun;39(3):165-7.
• [7] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 245).