Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTX3HNZ)

• DTT Name: Galanin receptor type 1 (GAL1-R)
• Synonyms: GALR1; GALR-1; GALNR1; GALN1R; GAL1-R
• Gene Name: GALR1
• DTT Type: Literature-reported target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: GALR1_HUMAN
• TTD ID: T78581
• Sequence:
  MELAVGNLSEGNASWPEPPAPEPGPLFGIGVENFVTLVVFGLIFALGVLGNSLVITVLAR
  SKPGKPRSTTNLFILNLSIADLAYLLFCIPFQATVYALPTWVLGAFICKFIHYFFTVSML
  VSIFTLAAMSVDRYVAIVHSRRSSSLRVSRNALLGVGCIWALSIAMASPVAYHQGLFHPR
  ASNQTFCWEQWPDPRHKKAYVVCTFVFGYLLPLLLICFCYAKVLNHLHKKLKNMSKKSEA
  SKKKTAQTVLVVVVVFGISWLPHHIIHLWAEFGVFPLTPASFLFRITAHCLAYSNSSVNP
  IIYAFLSENFRKAYKQVFKCHIRKDSHLSDTKESKSRIDTPPSTNCTHV
• Function: The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity. Receptor for the hormone galanin. G protein-coupled peptide receptor activity. Neuropeptide binding. Peptide hormone binding.
• 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

26 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(Sar)WTLNSAGYLLGPKK(Lys-decanoyl)K	DMJL8SE	Discovery agent	N.A.	Investigative	[2]
(Sar)WTLNSAGYLLGPKK(Lys-lauroyl)K	DMPZHIE	Discovery agent	N.A.	Investigative	[2]
(Sar)WTLNSAGYLLGPKK(Lys-MPEG4)K	DMQIHZU	Discovery agent	N.A.	Investigative	[2]
(Sar)WTLNSAGYLLGPKK(Lys-myristoyl)K	DMVHDF4	Discovery agent	N.A.	Investigative	[2]
(Sar)WTLNSAGYLLGPKK(Lys-octanoyl)K	DMX3K4E	Discovery agent	N.A.	Investigative	[2]
(Sar)WTLNSAGYLLGPKK(Lys-palmitoyl)K	DMSVMI8	Discovery agent	N.A.	Investigative	[2]
(Sar)WTLNSAGYLLGPKK(Lys-stearoyl)K	DMO6N7C	Discovery agent	N.A.	Investigative	[2]
(Sar)WTLNSAGYLLGPKKKK	DMT2NVG	Discovery agent	N.A.	Investigative	[2]
Gal-B5	DM7PR5E	Discovery agent	N.A.	Investigative	[3]
GALANIN	DMHPV8A	Discovery agent	N.A.	Investigative	[4]
GALANTIDE	DMDZHEO	Discovery agent	N.A.	Investigative	[3]
GalB2	DMGX6UH	Discovery agent	N.A.	Investigative	[3]
Galnon	DMB8HCW	Discovery agent	N.A.	Investigative	[5]
GWTLNSAGYLLGPHAV-NH2	DMZPRIG	Discovery agent	N.A.	Investigative	[6]
GwTLNSAGYLLGPHAVGNHRSFSDKNGLTS-CONH2	DMPIRE0	Discovery agent	N.A.	Investigative	[3]
GWTLNSAGYLLGPPPALALA-CONH2	DMKFMQ5	Discovery agent	N.A.	Investigative	[3]
GWTLNSAGYLLGPPPGFSPFR-CONH2	DMVWGM2	Discovery agent	N.A.	Investigative	[3]
GWTLNSAGYLLGPRHYINLITRQRY-CONH2	DM5YR4S	Discovery agent	N.A.	Investigative	[3]
GWTLNSAGYLLGPrPKPQQwFwLL-CONH2	DM48AV3	Discovery agent	N.A.	Investigative	[3]
NAX-5055	DMO6T9C	Epileptic seizures	8A61-8A6Z	Investigative	[1]
WTLNSAGYLL-CONH2	DMF9SOV	Discovery agent	N.A.	Investigative	[3]
WTLNSAGYLLGPHAVGNHPSFSDKNGLTS-CONH2	DMB3567	Discovery agent	N.A.	Investigative	[3]
[N-Ac,des-Sar]Gal-B2	DMW6LIJ	Discovery agent	N.A.	Investigative	[3]
[N-Me,des-Sar]Gal-B2	DM4XFOH	Discovery agent	N.A.	Investigative	[3]
[Sar1Ala]GAL-B2	DMUD0LA	Discovery agent	N.A.	Investigative	[3]
[Sar1Gly]GAL-B2	DMUI0XV	Discovery agent	N.A.	Investigative	[3]

References

• [1] Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43.
• [2] Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues. J Med Chem. 2009 Mar 12;52(5):1310-6.
• [3] Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic de... J Med Chem. 2010 Feb 25;53(4):1871-5.
• [4] cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
• [5] Anticonvulsant activity of a nonpeptide galanin receptor agonist. Proc Natl Acad Sci U S A. 2002 May 14;99(10):7136-41.
• [6] Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities. J Med Chem. 2008 Dec 25;51(24):8038-47.