Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00394

Target Information
NameSomatostatin receptor type 2    
Type of targetSuccessful target    
SynonymsSRIF-1    
SS2R    
Somatostatin receptor 2    
Sst(2)    
DiseaseCancer, unspecified
[ICD9: 140-229   ICD10: C00-C96]
[1]
Cushing's disease
[ICD9: 255.0   ICD10: E24.0]
[1]
Neuroblastoma
[ICD9: 194.0   ICD10: C74.9]
[1]
Drug(s)OctreotideApprovedAcromegaly[2]
Lanreotide AutogelMarketedAcromegaly[3]
PasireotidePhase IIIPancreatic Cancer[3]
BIM23A760Phase IIAcromegaly[4]
PasireotidePhase INeuroendocrine Tumor; Carcinoid Tumor; Pancreatic Neuroendocrine Tumor[3]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP30874
FunctionReceptor for somatostatins-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and plc via pertussis toxin insensitive as well as sensitive.    
SequenceMDMADEPLNGSHTWLSIPFDLNGSVVSTNTSNQTEPYYDLTSNAVLTFIYFVVCIIGLCG NTLVIYVILRYAKMKTITNIYILNLAIADELFMLGLPFLAMQVALVHWPFGKAICRVVMT VDGINQFTSIFCLTVMSIDRYLAVVHPIKSAKWRRPRTAKMITMAVWGVSLLVILPIMIY AGLRSNQWGRSSCTINWPGESGAWYTGFIIYTFILGFLVPLTIICLCYLFIIIKVKSSGI RVGSSKRKKSEKKVTRMVSIVVAVFIFCWLPFYIFNVSSVSMAISPTPALKGMFDFVVVL TYANSCANPILYAFLSDNFKKSFQNVLCLVKVSGTDDGERSDSKQDKSRLNETTETQRTL LNGDLQTSI
Related US Patent6,387,932
Target ValidationClick to Find Target Validation Information.    
InhibitorAla11-SRIF-14-amide[5]
Ala6-SRIF-14-amide[5]
Ala7-SRIF-14-amide[5]
CytotoxinPeptide Conjugate[6]
CytotoxinPeptide Conjugate[6]
CytotoxinPeptide Conjugate[6]
D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH2[7]
Des-AA1,2,4,12,13-[D-Trp8]SRIF[8]
Des-AA1,2,4,13-[D-Trp8]SRIF[8]
Des-AA1,2,4,5,11,12,13-[D-Trp8]SRIF[8]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF[8]
Des-AA1,2,4,5,6,12,13-[D-Trp8]SRIF[8]
Des-AA1,2,4,5-[D-Trp8]SRIF[8]
Des-AA1,2,5,12,13-[D-Trp8]SRIF[8]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF[9]
Des-AA5-[D-Trp8]SRIF[9]
Edotreotide[10]
H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2[7]
H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2[11]
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2[11]
H-c[Cys-Phe-DTrp-Lys-Thr-Cys]-OH[11]
L-363377[12]
ODT-8[8]
Pyz11-D-Trp8-SRIF[5]
Pyz6-D-Trp8-SRIF[5]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
Radiolabeled octreotide derivative[10]
SOMATOSTATIN[7]
SRIF-28[13]
Somatostatin Analogue[14]
Somatostatin Analogue[14]
Somatostatin Analogue[14]
Somatostatin Analogue[14]
AgonistL-054852[3]
Pasireotide[3]
AntagonistBIM23A760[4]
BinderLanreotide Autogel[3]
Octreotide[2]
MultitargetPasireotide[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Somatostatin receptor gene expression in neuroblastoma. Regul Pept. 2000 Mar 17;88(1-3):61-73. To Reference
Ref 2Versatile conjugation of octreotide to dendrimers by cycloaddition ("click") chemistry to yield high-affinity multivalent cyclic Peptide dendrimers. Bioconjug Chem. 2009 Jul;20(7):1323-31. To Reference
Ref 3Treatment strategies for acromegaly. Expert Opin Emerg Drugs. 2005 Nov;10(4):875-90. To Reference
Ref 4Emerging drugs for acromegaly. Expert Opin Emerg Drugs. 2008 Jun;13(2):273-93. To Reference
Ref 5J Med Chem. 2005 Jun 16;48(12):4025-30.Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4. An unexpected effect of the chirality of Trp8 on NMR spectra in methanol. To Reference
Ref 6Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates. To Reference
Ref 7J 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 8J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. To Reference
Ref 9J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. To Reference
Ref 10J 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. To Reference
Ref 11J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR. To Reference
Ref 12J Med Chem. 1998 Jun 18;41(13):2175-9.Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists. 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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