Target Information

Target General Infomation
Target ID
T13453
Former ID
TTDR01044
Target Name
Galanin receptortype 2
Gene Name
GALR2
Synonyms
GAL2-R; GALR2
Target Type
Research
Function
Receptor for thehormone galanin and GALP. Receptor for the hormone spexin-1 (PubMed:24517231). 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)).
BioChemical Class
GPCR rhodopsin
Target Validation
T13453
UniProt ID
O43603
Sequence
MNVSGCPGAGNASQAGGGGGWHPEAVIVPLLFALIFLVGTVGNTLVLAVLLRGGQAVSTT
NLFILNLGVADLCFILCCVPFQATIYTLDGWVFGSLLCKAVHFLIFLTMHASSFTLAAVS
LDRYLAIRYPLHSRELRTPRNALAAIGLIWGLSLLFSGPYLSYYRQSQLANLTVCHPAWS
APRRRAMDICTFVFSYLLPVLVLGLTYARTLRYLWRAVDPVAAGSGARRAKRKVTRMILI
VAALFCLCWMPHHALILCVWFGQFPLTRATYALRILSHLVSYANSCVNPIVYALVSKHFR
KGFRTICAGLLGRAPGRASGRVCAAARGTHSGSVLERESSDLLHMSEAAGALRPCPGASQ
PCILEPCPGPSWQGPKAGDSILTVDVA
Inhibitor (Sar)WTLNSAGYLLGPKK(Lys-decanoyl)K Drug Info [529952]
(Sar)WTLNSAGYLLGPKK(Lys-lauroyl)K Drug Info [529952]
(Sar)WTLNSAGYLLGPKK(Lys-MPEG4)K Drug Info [529952]
(Sar)WTLNSAGYLLGPKK(Lys-myristoyl)K Drug Info [529952]
(Sar)WTLNSAGYLLGPKK(Lys-octanoyl)K Drug Info [529952]
(Sar)WTLNSAGYLLGPKK(Lys-palmitoyl)K Drug Info [529952]
(Sar)WTLNSAGYLLGPKK(Lys-stearoyl)K Drug Info [529952]
(Sar)WTLNSAGYLLGPKKKK Drug Info [529952]
Gal-B5 Drug Info [530680]
GALANIN Drug Info [529569]
GALANTIDE Drug Info [530680]
GalB2 Drug Info [530680]
GWTLNSAGYLLGPHAV-NH2 Drug Info [529837]
GwTLNSAGYLLGPHAVGNHRSFSDKNGLTS-CONH2 Drug Info [530680]
GWTLNSAGYLLGPPPALALA-CONH2 Drug Info [530680]
GWTLNSAGYLLGPPPGFSPFR-CONH2 Drug Info [530680]
GWTLNSAGYLLGPRHYINLITRQRY-CONH2 Drug Info [530680]
GWTLNSAGYLLGPrPKPQQwFwLL-CONH2 Drug Info [530680]
WTLNSAGYLL-CONH2 Drug Info [530680]
WTLNSAGYLLGPHAVGNHPSFSDKNGLTS-CONH2 Drug Info [530680]
[N-Ac,des-Sar]Gal-B2 Drug Info [530680]
[N-Me,des-Sar]Gal-B2 Drug Info [530680]
[Sar1Ala]GAL-B2 Drug Info [530680]
[Sar1Gly]GAL-B2 Drug Info [530680]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Reactome Peptide ligand-binding receptors
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 529569J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
Ref 529837J Med Chem. 2008 Dec 25;51(24):8038-47.Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities.
Ref 529952J Med Chem. 2009 Mar 12;52(5):1310-6.Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.

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