Therapeutic Targets Database
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TTD Target ID: TTDC00034

Target Information
NameSomatostatin receptor type 4    
Type of targetClinical trial target    
SynonymsSS4R    
SSTR4    
DiseaseSolid tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[1][2]
Drug(s)CAP-232Phase IIa completedRefractory Renal Cell Carcinoma[3][1][2]
CAP-232Phase IISolid Tumors[3][1][2]
PathwayNeuroactive ligand-receptor interaction
UniProt IDP31391
SequenceMSAPSTLPPGGEEGLGTAWPSAANASSAPAEAEEAVAGPGDARAAGMVAIQCIYALVCLV GLVGNALVIFVILRYAKMKTATNIYLLNLAVADELFMLSVPFVASSAALRHWPFGSVLCR AVLSVDGLNMFTSVFCLTVLSVDRYVAVVHPLRAATYRRPSVAKLINLGVWLASLLVTLP IAIFADTRPARGGQAVACNLQWPHPAWSAVFVVYTFLLGFLLPVLAIGLCYLLIVGKMRA VALRAGWQQRRRSEKKITRLVLMVVVVFVLCWMPFYVVQLLNLFVTSLDATVNHVSLILS YANSCANPILYGFLSDNFRRFFQRVLCLRCCLLEGAGGAEEEPLDYYATALKSKGGAGCM CPPLPCQQEALQPEPGRKRIPLTRTTTF
Target ValidationClick to Find Target Validation Information.    
InhibitorAla11-SRIF-14-amide[4]
Ala6-SRIF-14-amide[4]
CytotoxinPeptide Conjugate[5]
CytotoxinPeptide Conjugate[5]
CytotoxinPeptide Conjugate[5]
D-Trp8-SRIF-14[4]
Des-AA1,2,4,12,13-[D-Trp8]SRIF[6]
Des-AA1,2,4,13-[D-Trp8]SRIF[6]
Des-AA1,2,4,5,10,12,13-[D-Trp8]SRIF[6]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF[6]
Des-AA1,2,4,5,6,12,13-[D-Trp8]SRIF[6]
Des-AA1,2,4,5-[D-Trp8]SRIF[6]
Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF[6]
Des-AA1,2,5,12,13-[D-Trp8]SRIF[6]
Des-AA1,2,5-[D-Nal8,IAmp9, (NalphaMe)Thr12]SRIF[7]
Des-AA1,2,5-[D-Trp8, (NalphaMe)IAmp9]SRIF[7]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF[7]
Des-AA1,2,5-[IAmp9,Tyr11]-SRIF[7]
Des-AA1,5-[Tyr2,D-Trp8, (NalphaMe)IAmp9]Cbm-SRIF[7]
Des-AA1,5-[Tyr2,D-Trp8, (NalphaMe)IAmp9]SRIF[7]
Des-AA5-[D-Trp8]SRIF[7]
ODT-8[6]
Pyz11-D-Trp8-SRIF[4]
Pyz6-D-Trp8-SRIF[4]
Pyz7-D-Trp8-SRIF[4]
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[9]
SRIF-28[10]
Somatostatin Analogue[11]
Somatostatin Analogue[11]
Somatostatin Analogue[11]
Somatostatin Analogue[11]
AgonistCAP-232[3][1][2]
MultitargetCAP-232[3][1][2]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Continuous 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 2Inhibitory 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 3TT-232: Somatostatin sst1/sst4 receptor agonist treatment of neuropathic pain treatment of inflammation. Drugs of the future. 2005; 30:558-66 To Reference
Ref 4J 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 5Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates. 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. 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 10J 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 11J 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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