Target Information
Target General Infomation | |||||
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Target ID |
T16633
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Former ID |
TTDC00112
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Target Name |
Somatostatin receptor 1
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Gene Name |
SSTR1
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Synonyms |
SRIF-2; SS1R; Somatostatin receptor 1; Sst(1); SSTR1
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Target Type |
Successful
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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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T16633
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UniProt ID | |||||
Sequence |
MFPNGTASSPSSSPSPSPGSCGEGGGSRGPGAGAADGMEEPGRNASQNGTLSEGQGSAIL
ISFIYSVVCLVGLCGNSMVIYVILRYAKMKTATNIYILNLAIADELLMLSVPFLVTSTLL RHWPFGALLCRLVLSVDAVNMFTSIYCLTVLSVDRYVAVVHPIKAARYRRPTVAKVVNLG VWVLSLLVILPIVVFSRTAANSDGTVACNMLMPEPAQRWLVGFVLYTFLMGFLLPVGAIC LCYVLIIAKMRMVALKAGWQQRKRSERKITLMVMMVVMVFVICWMPFYVVQLVNVFAEQD DATVSQLSVILGYANSCANPILYGFLSDNFKRSFQRILCLSWMDNAAEEPVDYYATALKS RAYSVEDFQPENLESGGVFRNGTCTSRITTL |
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Drugs and Mode of Action | |||||
Modulator | 99mTc-MIP-1407 | Drug Info | [530618], [532210] | ||
FR-121196 | Drug Info | [530618], [532210] | |||
Agonist | CGP 23996 | Drug Info | [525652] | ||
L-797,591 | Drug Info | [534729] | |||
L-817,818 | Drug Info | [534729] | |||
SRIF-14 | Drug Info | [534701] | |||
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-AA1,2,4,5,13-[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-[(NalphaMe)Cys3,D-Nal8,IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[(NalphaMe)Cys3,D-Trp8,IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[(NalphaMe)D-Nal8,IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[(NalphaMe)Lys4,D-Nal8,IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9,Tyr11]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Cys14]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Phe11]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Ser13]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Thr12]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Nal8,IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9,Tyr11]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Cys14]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Ser13]SRIF | Drug Info | [527384] | |||
Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Thr12]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,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-AA1,2,5-[IAmp9,Tyr11]-SRIF | Drug Info | [527384] | |||
Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF | Drug Info | [527385] | |||
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]Cbm-SRIF | Drug Info | [527384] | |||
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]SRIF | Drug Info | [527384] | |||
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF | Drug Info | [527384] | |||
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]SRIF CH-288 | Drug Info | [527385] | |||
Des-AA5-[D-Trp8]SRIF | Drug Info | [527384] | |||
ODT-8 | Drug Info | [527385] | |||
Pasireotide | Drug Info | [543787] | |||
SOMATOSTATIN | Drug Info | [527802] | |||
SRIF-28 | Drug Info | [531062] | |||
Antagonist | SRA880 | Drug Info | [527071] | ||
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 523209 | ClinicalTrials.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 525297 | ClinicalTrials.gov (NCT02527993) Treatment of Hypoglycemia Following Gastric Bypass Surgery. | ||||
Ref 525652 | Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn Schmiedebergs Arch Pharmacol. 1999 Nov;360(5):488-99. | ||||
Ref 526564 | Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates. | ||||
Ref 527071 | SRA880, in vitro characterization of the first non-peptide somatostatin sst(1) receptor antagonist. Neurosci Lett. 2004 May 6;361(1-3):132-5. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527802 | J 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 530618 | Mol Endocrinol. 2010 Feb;24(2):436-46. Epub 2010 Jan 5.Pasireotide and octreotide stimulate distinct patterns of sst2A somatostatin receptor phosphorylation. | ||||
Ref 531062 | J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. | ||||
Ref 534701 | Synthesis 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. |
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