Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00253

Target Information
NameSomatostatin receptor type 5    
Type of targetClinical trial target    
SynonymsSS5R    
DiseaseCushing's disease
[ICD9: 255.0   ICD10: E24.0]
[1][2]
Drug(s)PasireotidePhase IIIPancreatic Cancer[3]
PasireotidePhase INeuroendocrine Tumor; Carcinoid Tumor; Pancreatic Neuroendocrine Tumor[3]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP35346
FunctionReceptor for somatostatin 28 and to a lesser extent for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.    
SequenceMEPLFPASTPSWNASSPGAASGGGDNRTLVGPAPSAGARAVLVPVLYLLVCAAGLGGNTL VIYVVLRFAKMKTVTNIYILNLAVADVLYMLGLPFLATQNAASFWPFGPVLCRLVMTLDG VNQFTSVFCLTVMSVDRYLAVVHPLSSARWRRPRVAKLASAAAWVLSLCMSLPLLVFADV QEGGTCNASWPEPVGLWGAVFIIYTAVLGFFAPLLVICLCYLLIVVKVRAAGVRVGCVRR RSERKVTRMVLVVVLVFAGCWLPFFTVNIVNLAVALPQEPASAGLYFFVVILSYANSCAN PVLYGFLSDNFRQSFQKVLCLRKGSGAKDADATEPRPDRIRQQQEATPPAHRAAANGLMQ TSKL//
Target ValidationClick to Find Target Validation Information.    
InhibitorCytotoxinPeptide Conjugate[4]
CytotoxinPeptide Conjugate[4]
CytotoxinPeptide Conjugate[4]
D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH2[5]
Des-AA1,2,4,12,13-[D-Trp8]SRIF[6]
Des-AA1,2,4,13-[D-Trp8]SRIF[6]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF[6]
Des-AA1,2,4,5-[D-Trp8]SRIF[6]
Des-AA1,2,5,12,13-[D-Trp8]SRIF[6]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF[7]
Des-AA5-[D-Trp8]SRIF[7]
Edotreotide[8]
H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2[5]
H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2[9]
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2[9]
ODT-8[6]
PTR-3046[10]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
Radiolabeled octreotide derivative[8]
SOMATOSTATIN[5]
SRIF-28[11]
Somatostatin Analogue[12]
Somatostatin Analogue[12]
Somatostatin Analogue[12]
Somatostatin Analogue[12]
AgonistPasireotide[3]
MultitargetPasireotide[3]
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 3Treatment strategies for acromegaly. Expert Opin Emerg Drugs. 2005 Nov;10(4):875-90. To Reference
Ref 4Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates. To Reference
Ref 5J 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 6J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. To Reference
Ref 7J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. To Reference
Ref 8J 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 9J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR. To Reference
Ref 10J Med Chem. 2009 Jan 8;52(1):95-104.Highly potent 4-amino-indolo[2,3-c]azepin-3-one-containing somatostatin mimetics with a range of sst receptor selectivities. To Reference
Ref 11J 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 12J 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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