Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTBPW3J)

• DTT Name: Galanin receptor type 2 (GAL2-R)
• Synonyms: GALR2; GALR-2; GALNR2; GAL2-R
• Gene Name: GALR2
• DTT Type: Literature-reported target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: GALR2_HUMAN
• TTD ID: T13453
• Sequence:
  MNVSGCPGAGNASQAGGGGGWHPEAVIVPLLFALIFLVGTVGNTLVLAVLLRGGQAVSTT
  NLFILNLGVADLCFILCCVPFQATIYTLDGWVFGSLLCKAVHFLIFLTMHASSFTLAAVS
  LDRYLAIRYPLHSRELRTPRNALAAIGLIWGLSLLFSGPYLSYYRQSQLANLTVCHPAWS
  APRRRAMDICTFVFSYLLPVLVLGLTYARTLRYLWRAVDPVAAGSGARRAKRKVTRMILI
  VAALFCLCWMPHHALILCVWFGQFPLTRATYALRILSHLVSYANSCVNPIVYALVSKHFR
  KGFRTICAGLLGRAPGRASGRVCAAARGTHSGSVLERESSDLLHMSEAAGALRPCPGASQ
  PCILEPCPGPSWQGPKAGDSILTVDVA
• Function: The activity of this receptor is mediated by G proteins that activate the phospholipase C/protein kinase C pathway (via G(q)) and that inhibit adenylyl cyclase (via G(i)). Receptor for the hormone galanin and GALP. 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

24 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	[1]
GALANIN	DMHPV8A	Discovery agent	N.A.	Investigative	[3]
GALANTIDE	DMDZHEO	Discovery agent	N.A.	Investigative	[1]
GalB2	DMGX6UH	Discovery agent	N.A.	Investigative	[1]
GWTLNSAGYLLGPHAV-NH2	DMZPRIG	Discovery agent	N.A.	Investigative	[4]
GwTLNSAGYLLGPHAVGNHRSFSDKNGLTS-CONH2	DMPIRE0	Discovery agent	N.A.	Investigative	[1]
GWTLNSAGYLLGPPPALALA-CONH2	DMKFMQ5	Discovery agent	N.A.	Investigative	[1]
GWTLNSAGYLLGPPPGFSPFR-CONH2	DMVWGM2	Discovery agent	N.A.	Investigative	[1]
GWTLNSAGYLLGPRHYINLITRQRY-CONH2	DM5YR4S	Discovery agent	N.A.	Investigative	[1]
GWTLNSAGYLLGPrPKPQQwFwLL-CONH2	DM48AV3	Discovery agent	N.A.	Investigative	[1]
WTLNSAGYLL-CONH2	DMF9SOV	Discovery agent	N.A.	Investigative	[1]
WTLNSAGYLLGPHAVGNHPSFSDKNGLTS-CONH2	DMB3567	Discovery agent	N.A.	Investigative	[1]
[N-Ac,des-Sar]Gal-B2	DMW6LIJ	Discovery agent	N.A.	Investigative	[1]
[N-Me,des-Sar]Gal-B2	DM4XFOH	Discovery agent	N.A.	Investigative	[1]
[Sar1Ala]GAL-B2	DMUD0LA	Discovery agent	N.A.	Investigative	[1]
[Sar1Gly]GAL-B2	DMUI0XV	Discovery agent	N.A.	Investigative	[1]

References

• [1] 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.
• [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] Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.
• [4] 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.