Target Information

Target General Infomation
Target ID
T78581
Former ID
TTDR00184
Target Name
Galanin receptor type 1
Gene Name
GALR1
Synonyms
GAL1-R; GALR1
Target Type
Research
Disease Epileptic seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Function
Receptor for the hormone galanin. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity.
BioChemical Class
GPCR rhodopsin
Target Validation
T78581
UniProt ID
P47211
Sequence
MELAVGNLSEGNASWPEPPAPEPGPLFGIGVENFVTLVVFGLIFALGVLGNSLVITVLAR
SKPGKPRSTTNLFILNLSIADLAYLLFCIPFQATVYALPTWVLGAFICKFIHYFFTVSML
VSIFTLAAMSVDRYVAIVHSRRSSSLRVSRNALLGVGCIWALSIAMASPVAYHQGLFHPR
ASNQTFCWEQWPDPRHKKAYVVCTFVFGYLLPLLLICFCYAKVLNHLHKKLKNMSKKSEA
SKKKTAQTVLVVVVVFGISWLPHHIIHLWAEFGVFPLTPASFLFRITAHCLAYSNSSVNP
IIYAFLSENFRKAYKQVFKCHIRKDSHLSDTKESKSRIDTPPSTNCTHV
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 [529789]
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]
Agonist Galnon Drug Info [535451]
NAX-5055 Drug Info [536934]
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 529789J Med Chem. 2008 Nov 27;51(22):7094-8.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 responses against carrageenan-induced hyperalgesia.
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.
Ref 535451Anticonvulsant activity of a nonpeptide galanin receptor agonist. Proc Natl Acad Sci U S A. 2002 May 14;99(10):7136-41.
Ref 536934Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43. Epub 2008 Nov 12.

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