90 articles for thisTarget
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Article Title
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SAR exploration at the C-3 position of tetrahydro-ß-carboline sstr3 antagonists.
Merck Research Laboratories
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Merck Research Laboratories
Treating pain with somatostatin receptor subtype 4 agonists.
Therachem Research Medilab (India)
Investigation of Cardiovascular Effects of Tetrahydro-ß-carboline sstr3 antagonists.
Merck Research Laboratories
Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.
Merck Research Laboratories
Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor.
Novartis Institutes For Biomedical Research
SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.
Novartis Institutes For Biomedical Research
Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists.
Novartis Institutes For Biomedical Research
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.
TBA
Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.
TBA
N-Methylated sst2 Selective Somatostatin Cyclic Peptide Analogue as a Potent Candidate for Treating Neurogenic Inflammation.
TBA
Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors.
University of Firenze
Novel, potent, and radio-iodinatable somatostatin receptor 1 (sst1) selective analogues.
The Clayton Foundation Laboratories For Peptide Biology
Highly potent 4-amino-indolo[2,3-c]azepin-3-one-containing somatostatin mimetics with a range of sst receptor selectivities.
Vrije Universiteit Brussel
Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.
University of Berne
Ring size of somatostatin analogues (ODT-8) modulates receptor selectivity and binding affinity.
Salk Institute
Ring size in octreotide amide modulates differently agonist versus antagonist binding affinity and selectivity.
Salk Institute
Novel sst5-selective somatostatin dicarba-analogues: synthesis and conformation-affinity relationships.
University of Firenze
Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from rat pituitary cells.
University of California San Diego
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.
Technische Universit£T M£Nchen
Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.
Salk Institute
Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
Salk Institute
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
Merck Research Laboratories
Highly potent and subtype selective ligands derived by N-methyl scan of a somatostatin antagonist.
Tulane University Health Sciences Center
Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity.
Institut Henri Beaufour
Potent antagonists of somatostatin: synthesis and biology.
Tulane University School of Medicine
Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists.
Merck Research Laboratories
Synthesis of substituted imidazopyrazines as ligands for the human somatostatin receptor subtype 5.
Institut Henri Beaufour
N-imidazolebenzyl-histidine substitution in somatostatin and in its octapeptide analogue modulates receptor selectivity and function.
Salk Institute
Biological diversity from a structurally diverse library: systematically scanning conformational space using a pyranose scaffold.
Alchemia
Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.
F. Hoffmann-La Roche
From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.
F. Hoffmann-La Roche
Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.
F. Hoffmann-La Roche
New sst4/5-selective somatostatin peptidomimetics based on a constrained tryptophan scaffold.
Vrije Universiteit Brussel
Side Chain Cyclized Aromatic Amino Acids: Great Tools as Local Constraints in Peptide and Peptidomimetic Design.
Vrije Universiteit Brussel
Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
Salk Institute
Synthesis and structure-activity relationships of 3,4,5-trisubstituted-1,2,4-triazoles: high affinity and selective somatostatin receptor-4 agonists for Alzheimer's disease treatment.
Southern Illinois University Edwardsville
Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism.
Crinetics Pharmaceuticals
Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Salk Institute
Novel sst(4)-selective somatostatin (SRIF) agonists. 4. Three-dimensional consensus structure by NMR.
Salk Institute
Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.
Salk Institute
Urolinin: The First Linear Peptidic Urotensin-II Receptor Agonist.
Charit£-Universit£Tsmedizin Berlin
Human somatostatin receptor specificity of backbone-cyclic analogues containing novel sulfur building units.
Hebrew University
Discovery of substituted 3H-pyrido[2,3-d]pyrimidin-4-ones as potent, biased, and orally bioavailable sst2 agonist.
Crinetics Pharmaceuticals
Potent somatostatin undecapeptide agonists selective for somatostatin receptor 1 (sst1).
Salk Institute
N-Methyl scan of somatostatin octapeptide agonists produces interesting effects on receptor subtype specificity.
Tulane University Health Sciences Center
Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation.
University of California
Discovery of an SSTR2-Targeting Maytansinoid Conjugate (PEN-221) with Potent Activity in Vitro and in Vivo.
Tarveda Therapeutics
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.
Merck Research Laboratories
Highly potent cyclic disulfide antagonists of somatostatin.
Tulane University School of Medicine
Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.
Merck Research Laboratories
Design, synthesis, and biological activities of potent and selective somatostatin analogues incorporating novel peptoid residues.
University of California San Diego
Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.
University of Pennsylvania
[DOTA]Somatostatin-14 analogs and their (111)In-radioligands: effects of decreasing ring-size on sst1-5 profile, stability and tumor targeting.
Inrastes
A tetradecapeptide somatostatin dicarba-analog: Synthesis, structural impact and biological activity.
Institute For Research In Biomedicine (Irb Barcelona)
A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential.
Novartis Pharma
Peptide folding induces high and selective affinity of a linear and small beta-peptide to the human somatostatin receptor 4.
Eth Zurich
Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.
Merck
Design and synthesis of a novel series of orally active, selective somatostatin receptor 2 agonists for the treatment of type 2 diabetes.
Takeda Pharmaceutical
Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806.
University of Cambridge
Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Novartis Pharma
Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.
Merck Research Laboratories
The elucidation of somatostatin receptor functions: a current view.
German Institute of Human Nutrition
The somatostatin analog octreotide as potential treatment for re-stenosis and chronic rejection.
Novartis Pharma Research
Differential expression of multiple somatostatin receptors in the rat cerebellum during development.
Dynamique Des Systemes Neuroendocriniens
Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation.
Cedars-Sinai Research Institute
Identification and characterization of novel somatostatin antagonists.
Cyenamid Agricultural Research Center
Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
University of Pennsylvania
Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Mcgill University
Characterization of somatostatin receptor subtypes controlling rat gastric acid and pancreatic amylase release.
Tulane University