Target Information

Target General Infomation
Target ID
T16633
Former ID
TTDC00112
Target Name
Somatostatin receptor 1
Gene Name
SSTR1
Synonyms
SRIF-2; SS1R; Somatostatin receptor 1; Sst(1); SSTR1
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 with higher affinity for somatostatin-14 than -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphataseand Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins.
BioChemical Class
GPCR rhodopsin
Target Validation
T16633
UniProt ID
P30872
Sequence
MFPNGTASSPSSSPSPSPGSCGEGGGSRGPGAGAADGMEEPGRNASQNGTLSEGQGSAIL
ISFIYSVVCLVGLCGNSMVIYVILRYAKMKTATNIYILNLAIADELLMLSVPFLVTSTLL
RHWPFGALLCRLVLSVDAVNMFTSIYCLTVLSVDRYVAVVHPIKAARYRRPTVAKVVNLG
VWVLSLLVILPIVVFSRTAANSDGTVACNMLMPEPAQRWLVGFVLYTFLMGFLLPVGAIC
LCYVLIIAKMRMVALKAGWQQRKRSERKITLMVMMVVMVFVICWMPFYVVQLVNVFAEQD
DATVSQLSVILGYANSCANPILYGFLSDNFKRSFQRILCLSWMDNAAEEPVDYYATALKS
RAYSVEDFQPENLESGGVFRNGTCTSRITTL
Drugs and Mode of Action
Drug(s) Pasireotide Drug Info Approved Cushing's disease [1], [2]
ODT-8 Drug Info Phase 3 Discovery agent [3]
FR-121196 Drug Info Terminated Alzheimer disease [4]
Modulator 99mTc-MIP-1407 Drug Info [5], [6]
FR-121196 Drug Info [5], [6]
Agonist CGP 23996 Drug Info [7]
L-797,591 Drug Info [8]
L-817,818 Drug Info [8]
SRIF-14 Drug Info [9]
Inhibitor CytotoxinPeptide Conjugate Drug Info [10]
Des-AA1,2,4,12,13-[D-Trp8]SRIF Drug Info [11]
Des-AA1,2,4,13-[D-Trp8]SRIF Drug Info [11]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF Drug Info [11]
Des-AA1,2,4,5-[D-Trp8]SRIF Drug Info [11]
Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF Drug Info [11]
Des-AA1,2,5,12,13-[D-Trp8]SRIF Drug Info [11]
Des-AA1,2,5-[(NalphaMe)Cys3,D-Nal8,IAmp9]SRIF Drug Info [12]
Des-AA1,2,5-[(NalphaMe)Cys3,D-Trp8,IAmp9]SRIF Drug Info [12]
Des-AA1,2,5-[(NalphaMe)D-Nal8,IAmp9]SRIF Drug Info [12]
Des-AA1,2,5-[(NalphaMe)Lys4,D-Nal8,IAmp9]SRIF Drug Info [12]
Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9,Tyr11]SRIF Drug Info [12]
Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9]SRIF Drug Info [12]
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Cys14]SRIF Drug Info [12]
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Phe11]SRIF Drug Info [12]
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Ser13]SRIF Drug Info [12]
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Thr12]SRIF Drug Info [12]
Des-AA1,2,5-[D-Nal8,IAmp9]SRIF Drug Info [12]
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9,Tyr11]SRIF Drug Info [12]
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF Drug Info [12]
Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Cys14]SRIF Drug Info [12]
Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Ser13]SRIF Drug Info [12]
Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Thr12]SRIF Drug Info [12]
Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF Drug Info [12]
Des-AA1,2,5-[D-Trp8,IAmp9,Tyr11]Cbm-SRIF Drug Info [12]
Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275 Drug Info [12]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF Drug Info [12]
Des-AA1,2,5-[IAmp9,Tyr11]-SRIF Drug Info [12]
Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF Drug Info [11]
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]Cbm-SRIF Drug Info [12]
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]SRIF Drug Info [12]
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF Drug Info [12]
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]SRIF CH-288 Drug Info [11]
Des-AA5-[D-Trp8]SRIF Drug Info [12]
ODT-8 Drug Info [11]
Pasireotide Drug Info [13]
SOMATOSTATIN Drug Info [14]
SRIF-28 Drug Info [15]
Antagonist SRA880 Drug Info [16]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cAMP signaling 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 SIDS Susceptibility Pathways
GPCRs, Class A Rhodopsin-like
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
REF 1ClinicalTrials.gov (NCT02527993) Treatment of Hypoglycemia Following Gastric Bypass Surgery.
REF 2Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3ClinicalTrials.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 4Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001380)
REF 5Mol Endocrinol. 2010 Feb;24(2):436-46. Epub 2010 Jan 5.Pasireotide and octreotide stimulate distinct patterns of sst2A somatostatin receptor phosphorylation.
REF 6Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
REF 7Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn Schmiedebergs Arch Pharmacol. 1999 Nov;360(5):488-99.
REF 8Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40.
REF 9Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10836-41.
REF 10Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
REF 11J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
REF 12J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
REF 13(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: 355).
REF 14J 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 15J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors.
REF 16SRA880, in vitro characterization of the first non-peptide somatostatin sst(1) receptor antagonist. Neurosci Lett. 2004 May 6;361(1-3):132-5.

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