Target Validation Information
Target ID T62974
Target Name Somatostatin receptor type 4
Target Type
Clinical Trial
Drug Potency against Target Pyz11-D-Trp8-SRIF Drug Info Ki = 124 nM [527585]
Pyz6-D-Trp8-SRIF Drug Info Ki = 77 nM [527585]
Des-AA1,2,4,5,6,12,13-[D-Trp8]SRIF Drug Info IC50 = 229 nM [527385]
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]SRIF Drug Info IC50 = 245 nM [527384]
Des-AA1,2,4,13-[D-Trp8]SRIF Drug Info IC50 = 1.4 nM [527385]
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Thr12]SRIF Drug Info IC50 = 417 nM [527384]
Des-AA1,2,5-[IAmp9,Tyr11]-SRIF Drug Info IC50 = 384 nM [527384]
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]Cbm-SRIF Drug Info IC50 = 418 nM [527384]
SOMATOSTATIN Drug Info Ki = 1.7 nM [527802]
Des-AA5-[D-Trp8]SRIF Drug Info IC50 = 1.7 nM [527384]
CytotoxinPeptide Conjugate Drug Info IC50 = 2.79 nM [526564]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF Drug Info IC50 = 0.5 nM [527384]
Des-AA1,2,4,5,10,12,13-[D-Trp8]SRIF Drug Info IC50 = 786 nM [527385]
Ala11-SRIF-14-amide Drug Info Ki < 1 nM [527585]
Des-AA1,2,4,12,13-[D-Trp8]SRIF Drug Info IC50 = 1.2 nM [527385]
CAP-232 Drug Info IC50 = 0.1 nM
Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF Drug Info IC50 = 932 nM [527385]
SRIF-28 Drug Info IC50 = 1.6 nM [531062]
Ala6-SRIF-14-amide Drug Info Ki = 80 nM [527585]
Pyz7-D-Trp8-SRIF Drug Info Ki = 700 nM [527585]
D-Trp8-SRIF-14 Drug Info Ki = 3.7 nM [527585]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF Drug Info IC50 = 1 nM [527385]
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF Drug Info IC50 = 226 nM [527384]
ODT-8 Drug Info IC50 = 1.8 nM [527385]
Des-AA1,2,5,12,13-[D-Trp8]SRIF Drug Info IC50 = 0.6 nM [527385]
Des-AA1,2,4,5-[D-Trp8]SRIF Drug Info IC50 = 3.3 nM [527385]
Action against Disease Model TLN-4601 TLN-4601 potently inhibited the anchorage-dependent and -independent growth of KRAS-transformed h uMan nestin-positive (HPNE) pancreatic duct-derived cells. The growth of KRAS mutation-positive pancreatic carcinoma cell lines (PDAC) was inhibited by TLN-4601. [528944] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Functional experiments revealed no differences in intestinal motility or smooth muscle cell contractility between wild-type and somatostatin (SOM) receptor 4(SSTR4) knockout (SSTR4(-/-)) mice in physiological conditions. As revealed by multiple immunofluorescent labellings, RT-PCR and quantitative real time RT-PCR (qPCR), genetic deficiency of SSTR4 considerably altered the expression of SOM and SSTRs in non-inflamed and inflamed conditions, affecting both extrinsic and intrinsic components of the intestinal innervation, along with SSTR expression in several non-neuronalcell types. Moreover, substance P and calcitonin gene-related peptide expression were significantly elevated in SSTR4(-/-) mice, confirming the modulatory role of SSTR4 on intestinal pro-inflammatoryneuropeptide expression. These data suggest that SSTR4 plays a previously unexpected modulatory role in the regulation of intestinal SSTR expression. Moreover, in addition to the recently described inhibitory effects of SSTR4 on the neuronal release of pro-inflammatory peptides, SSTR4 appears also to be involved in the neuronal expression of both pro- and anti-inflammatory peptides in the murine small intestine [527585]
References
Ref 527585J 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.
Ref 527585J 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.
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 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 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
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 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 526564Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 528944Cancer Chemother Pharmacol. 2008 May;61(6):911-21. Epub 2007 Jul 11.Identification, characterization and potent antitumor activity of ECO-4601, a novel peripheral benzodiazepine receptor ligand.
Ref 527585J 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.
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 531062J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors.
Ref 527585J 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.
Ref 527585J 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.
Ref 527585J 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.
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 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.

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