Target Validation Information
Target ID T64830
Target Name Somatostatin receptor type 5
Target Type
Successful
Drug Potency against Target SRIF-28 Drug Info IC50 = 2.4 nM [531062]
PTR-3046 Drug Info IC50 = 67 nM [529856]
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2 Drug Info IC50 = 2.7 nM [528320]
H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 Drug Info Ki = 13.1 nM [527802]
Des-AA1,2,4,12,13-[D-Trp8]SRIF Drug Info IC50 = 31 nM [527385]
Des-AA5-[D-Trp8]SRIF Drug Info IC50 = 5 nM [527384]
D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH2 Drug Info IC50 = 5.6 nM [527802]
SOMATOSTATIN Drug Info IC50 = 0.2 nM [527802]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF Drug Info IC50 = 4.8 nM [527384]
Edotreotide Drug Info IC50 = 393 nM [527508]
CytotoxinPeptide Conjugate Drug Info IC50 = 2.79 nM [526564]
ODT-8 Drug Info IC50 = 46 nM [527385]
Des-AA1,2,4,13-[D-Trp8]SRIF Drug Info IC50 = 9.5 nM [527385]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF Drug Info IC50 = 43 nM [527385]
H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2 Drug Info IC50 = 158 nM [528320]
Radiolabeled octreotide derivative Drug Info IC50 = 10.8 nM [527508]
Des-AA1,2,5,12,13-[D-Trp8]SRIF Drug Info IC50 = 13 nM [527385]
Des-AA1,2,4,5-[D-Trp8]SRIF Drug Info IC50 = 8.6 nM [527385]
The Effect of Target Knockout, Knockdown or Genetic Variations To identify SSTR5-regulated pancreatic genes, gene expression microarray analysis was performed on the whole pancreas of 1- and 3-month-old wild-type (WT) and SSTR5 knockout (SSTR5-/-) male mice. Real-time RT-PCR and immunofluorescence were performed to validate selected differentially expressed genes.A set of 143 probes were identified to be differentially expressed in the pancreas of 1-month-old SSTR5-/- mice, 72 of which were downregulated and 71 upregulated. At 3 months of age, SSTR5 gene ablation resulted in downregulation of a set of 30 probes and upregulation of aset of 37 probes. Among these differentially expressed genes, there were 15 and 5 genes that were upregulated and downregulated, respectively, in mice at both 1 and 3 months of age. Three genes, PAP/INGAP, ANG, and TDE1, were selected to be validated by real-time RT-PCR and immunofluorescence. [531062]
References
Ref 531062J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors.
Ref 529856J 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.
Ref 528320J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
Ref 527802J 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 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 527802J 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 527802J 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 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 527508J 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.
Ref 526564Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 528320J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
Ref 527508J 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.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.

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