Target Information

Target General Infomation
Target ID
T13644
Former ID
TTDC00254
Target Name
Somatostatin receptor type 3
Gene Name
SSTR3
Synonyms
SS3R; SSR-28; SSTR3
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Cushing's disease [ICD9: 255; ICD10: E24.0]
Neuroendocrine cancer [ICD10: C7A]
Function
Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase.
BioChemical Class
GPCR rhodopsin
Target Validation
T13644
UniProt ID
P32745
Sequence
MDMLHPSSVSTTSEPENASSAWPPDATLGNVSAGPSPAGLAVSGVLIPLVYLVVCVVGLL
GNSLVIYVVLRHTASPSVTNVYILNLALADELFMLGLPFLAAQNALSYWPFGSLMCRLVM
AVDGINQFTSIFCLTVMSVDRYLAVVHPTRSARWRTAPVARTVSAAVWVASAVVVLPVVV
FSGVPRGMSTCHMQWPEPAAAWRAGFIIYTAALGFFGPLLVICLCYLLIVVKVRSAGRRV
WAPSCQRRRRSERRVTRMVVAVVALFVLCWMPFYVLNIVNVVCPLPEEPAFFGLYFLVVA
LPYANSCANPILYGFLSYRFKQGFRRVLLRPSRRVRSQEPTVGPPEKTEEEDEEEEDGEE
SREGGKGKEMNGRVSQITQPGTSGQERPPSRVASKEQQLLPQEASTGEKSSTMRISYL
Drugs and Mode of Action
Drug(s) Pasireotide Drug Info Approved Cushing's disease [525297], [551871]
ODT-8 Drug Info Phase 3 Discovery agent [523209]
FR-121196 Drug Info Terminated Alzheimer disease [544870]
Modulator 99mTc-MIP-1407 Drug Info [530618], [532210]
FR-121196 Drug Info [530618], [532210]
Agonist BN-81,644 Drug Info [526127]
BN-81,674 Drug Info [526127]
CGP 23996 Drug Info [525652]
L-796,778 Drug Info [534729]
SRIF-14 Drug Info [533890]
Inhibitor CytotoxinPeptide Conjugate Drug Info [526564]
Des-AA1,2,4,12,13-[D-Trp8]SRIF Drug Info [527385]
Des-AA1,2,4,13-[D-Trp8]SRIF Drug Info [527385]
Des-AA1,2,4,5,10,12,13-[D-Trp8]SRIF Drug Info [527385]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF Drug Info [527385]
Des-AA1,2,4,5-[D-Trp8]SRIF Drug Info [527385]
Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF Drug Info [527385]
Des-AA1,2,5,12,13-[D-Trp8]SRIF Drug Info [527385]
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF Drug Info [527384]
Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF Drug Info [527384]
Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275 Drug Info [527384]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF Drug Info [527384]
Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF Drug Info [527385]
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF Drug Info [527384]
Des-AA5-[D-Trp8]SRIF Drug Info [527384]
H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2 Drug Info [528320]
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2 Drug Info [528320]
ODT-8 Drug Info [527385]
Pasireotide Drug Info [543789]
Radiolabeled octreotide derivative Drug Info [527508]
SOMATOSTATIN Drug Info [527802]
SRIF-28 Drug Info [531062]
Antagonist NVP ACQ090 Drug Info [543789]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
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 523209ClinicalTrials.gov (NCT01220167) Three-way Crossover Comparative Water-effect Bioavailability to Compare Ondansetron ODFS 8mg With and Without Water With Zofran ODT 8mg Without Water in 18 Healthy Participants Under Fasting Conditions. U.S. National Institutes of Health.
Ref 525297ClinicalTrials.gov (NCT02527993) Treatment of Hypoglycemia Following Gastric Bypass Surgery.
Ref 544870Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001380)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525652Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn Schmiedebergs Arch Pharmacol. 1999 Nov;360(5):488-99.
Ref 526127Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity. J Med Chem. 2001 Aug 30;44(18):2990-3000.
Ref 526564Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527508J Med Chem. 2005 Apr 21;48(8):2778-89.N-terminal sugar conjugation and C-terminal Thr-for-Thr(ol) exchange in radioiodinated Tyr3-octreotide: effect on cellular ligand trafficking in vitro and tumor accumulation in vivo.
Ref 527802J Med Chem. 2005 Oct 20;48(21):6643-52.Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from rat pituitarycells.
Ref 528320J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
Ref 530618Mol Endocrinol. 2010 Feb;24(2):436-46. Epub 2010 Jan 5.Pasireotide and octreotide stimulate distinct patterns of sst2A somatostatin receptor phosphorylation.
Ref 531062J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 533890A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides. FEBS Lett. 1993 Apr 26;321(2-3):279-84.
Ref 534729Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40.
Ref 543789(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: 357).

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