97 articles for thisTarget
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An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
Tulane University Health Sciences Center
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
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.
University of Missouri
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
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
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.
University of Pennsylvania
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
Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.
University of Pennsylvania
Potent antagonists of somatostatin: synthesis and biology.
Tulane University School of Medicine
Nonpeptide somatostatin agonists with sst4 selectivity: synthesis and structure-activity relationships of thioureas.
Northeast Louisiana University
Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists.
Merck Research Laboratories
Lanthionine-somatostatin analogs: synthesis, characterization, biological activity, and enzymatic stability studies.
University of California San Diego
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 study of a somatostatin mimetic based on the 1-deoxynojrimycin scaffold.
Shandong University School of Medicine
Biological diversity from a structurally diverse library: systematically scanning conformational space using a pyranose scaffold.
Alchemia
Synthesis and anti-tumor activities of methyl 2-O-aryl-6-O-aryl'-D-glucopyranosides.
Ocean University of China
Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.
F. Hoffmann-La Roche
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.
Amgen
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
Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
Salk Institute
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
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
Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of somatostatin receptors. Correlation with the electrostatic potential of the substituents.
University of Pennsylvania
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
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
Ligand design for somatostatin receptor isoforms 4 and 5.
National University of Ireland Galway
Non-iminosugar glucocerebrosidase small molecule chaperones.
National Human Genome Research Institute
[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)
Somatostatin receptor-binding peptides suitable for tumor radiotherapy with Re-188 or Re-186. Chemistry and initial biological studies.
Diatide Research Laboaratories
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
Novel biphenyl bis-sulfonamides as acetyl and butyrylcholinesterase inhibitors: Synthesis, biological evaluation and molecular modeling studies.
Government College University
Design, Synthesis and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel DPP-4 Inhibitors.
China Pharmaceutical University
Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei.
Northeastern University
Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives.
Bezmialem Vakif University
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.
Pfizer
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.
Wyeth Research