Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00112

Target Information
NameSomatostatin receptor type 1    
Type of targetClinical trial target    
SynonymsSRIF-2    
SS1R    
Somatostatin receptor 1    
Sst(1)    
DiseaseCushing's disease
[ICD9: 255.0   ICD10: E24.0]
[1][2][3]
Neuroblastoma
[ICD9: 194.0   ICD10: C74.9]
[4]
Refractory Renal Cell Carcinoma
[ICD9: 189   ICD10: C64]
[5][6]
Drug(s)PasireotidePhase IIIPancreatic Cancer[7]
CAP-232Phase IIa completedRefractory Renal Cell Carcinoma[8][5][6]
CAP-232Phase IISolid Tumors[8][5][6]
PasireotidePhase INeuroendocrine Tumor; Carcinoid Tumor; Pancreatic Neuroendocrine Tumor[7]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP30872
FunctionReceptor 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 phosphatase and na(+)/h(+) exchange.    
SequenceMFPNGTASSPSSSPSPSPGSCGEGGGSRGPGAGAADGMEEPGRNASQNGTLSEGQGSAIL ISFIYSVVCLVGLCGNSMVIYVILRYAKMKTATNIYILNLAIADELLMLSVPFLVTSTLL RHWPFGALLCRLVLSVDAVNMFTSIYCLTVLSVDRYVAVVHPIKAARYRRPTVAKVVNLG VWVLSLLVILPIVVFSRTAANSDGTVACNMLMPEPAQRWLVGFVLYTFLMGFLLPVGAIC LCYVLIIAKMRMVALKAGWQQRKRSERKITLMVMMVVMVFVICWMPFYVVQLVNVFAEQD DATVSQLSVILGYANSCANPILYGFLSDNFKRSFQRILCLSWMDNAAEEPVDYYATALKS RAYSVEDFQPENLESGGVFRNGTCTSRITTL
Target ValidationClick to Find Target Validation Information.    
InhibitorCytotoxinPeptide Conjugate[9]
CytotoxinPeptide Conjugate[9]
CytotoxinPeptide Conjugate[9]
Des-AA1,2,4,12,13-[D-Trp8]SRIF[10]
Des-AA1,2,4,13-[D-Trp8]SRIF[10]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF[10]
Des-AA1,2,4,5-[D-Trp8]SRIF[10]
Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF[10]
Des-AA1,2,5,12,13-[D-Trp8]SRIF[10]
Des-AA1,2,5-[ (NalphaMe)Cys3,D-Nal8,IAmp9]SRIF[11]
Des-AA1,2,5-[ (NalphaMe)Cys3,D-Trp8,IAmp9]SRIF[11]
Des-AA1,2,5-[ (NalphaMe)D-Nal8,IAmp9]SRIF[11]
Des-AA1,2,5-[ (NalphaMe)Lys4,D-Nal8,IAmp9]SRIF[11]
Des-AA1,2,5-[D-Nal8, (NalphaMe)IAmp9,Tyr11]SRIF[11]
Des-AA1,2,5-[D-Nal8, (NalphaMe)IAmp9]SRIF[11]
Des-AA1,2,5-[D-Nal8,IAmp9, (NalphaMe)Cys14]SRIF[11]
Des-AA1,2,5-[D-Nal8,IAmp9, (NalphaMe)Phe11]SRIF[11]
Des-AA1,2,5-[D-Nal8,IAmp9, (NalphaMe)Ser13]SRIF[11]
Des-AA1,2,5-[D-Nal8,IAmp9, (NalphaMe)Thr12]SRIF[11]
Des-AA1,2,5-[D-Nal8,IAmp9]SRIF[11]
Des-AA1,2,5-[D-Trp8, (NalphaMe)IAmp9,Tyr11]SRIF[11]
Des-AA1,2,5-[D-Trp8, (NalphaMe)IAmp9]SRIF[11]
Des-AA1,2,5-[D-Trp8,IAmp9, (NalphaMe)Cys14]SRIF[11]
Des-AA1,2,5-[D-Trp8,IAmp9, (NalphaMe)Ser13]SRIF[11]
Des-AA1,2,5-[D-Trp8,IAmp9, (NalphaMe)Thr12]SRIF[11]
Des-AA1,2,5-[D-Trp8,IAmp9,Tyr11]Cbm-SRIF[11]
Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF[11]
Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275[11]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF[11]
Des-AA1,2,5-[IAmp9,Tyr11]-SRIF[11]
Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF[10]
Des-AA1,5-[Tyr2,D-Trp8, (NalphaMe)IAmp9]Cbm-SRIF[11]
Des-AA1,5-[Tyr2,D-Trp8, (NalphaMe)IAmp9]SRIF[11]
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF[11]
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]SRIF CH-288[10]
Des-AA5-[D-Trp8]SRIF[11]
ODT-8[10]
SOMATOSTATIN[12]
SRIF-28[13]
Somatostatin Analogue[14]
Somatostatin Analogue[14]
Somatostatin Analogue[14]
Somatostatin Analogue[14]
AgonistCAP-232[8][5][6]
Pasireotide[7]
MultitargetCAP-232[8][5][6]
Pasireotide[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The somatostatin analog SOM230 (pasireotide) ameliorates injury of the intestinal mucosa and increases survival after total-body irradiation by inhibiting exocrine pancreatic secretion. Radiat Res. 2009 Jun;171(6):698-707. To Reference
Ref 2Somatostatin analog octreotide LAR in gastro-entero-pancreatic tumors. Expert Rev Anticancer Ther. 2009 May;9(5):557-66. To Reference
Ref 3Current therapy and drug pipeline for the treatment of patients with acromegaly. Adv Ther. 2009 Apr;26(4):383-403. Epub 2009 May 4. To Reference
Ref 4Somatostatin receptor gene expression in neuroblastoma. Regul Pept. 2000 Mar 17;88(1-3):61-73. To Reference
Ref 5Continuous administration of the somatostatin structural derivative /TT-232/ by subcutaneously implanted osmotic pump improves the efficacy and potency of antitumor therapy in different mouse and human tumor models. Anticancer Res. 2008 Sep-Oct;28(5A):2769-74. To Reference
Ref 6Inhibitory effects of synthetic somatostatin receptor subtype 4 agonists on acute and chronic airway inflammation and hyperreactivity in the mouse. Eur J Pharmacol. 2008 Jan 14;578(2-3):313-22. Epub 2007 Oct 5. To Reference
Ref 7Treatment strategies for acromegaly. Expert Opin Emerg Drugs. 2005 Nov;10(4):875-90. To Reference
Ref 8TT-232: Somatostatin sst1/sst4 receptor agonist treatment of neuropathic pain treatment of inflammation. Drugs of the future. 2005; 30:558-66 To Reference
Ref 9Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates. To Reference
Ref 10J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. To Reference
Ref 11J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. To Reference
Ref 12J 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 pituitary cells. To Reference
Ref 13J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. To Reference
Ref 14J Med Chem. 1999 Apr 22;42(8):1341-7.Comparison of four 64Cu-labeled somatostatin analogues in vitro and in a tumor-bearing rat model: evaluation of new derivatives for positron emission tomography imaging and targeted radiotherapy. To Reference



 

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