74 articles for thisTarget
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Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy.
Washington University
Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
Washington University
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
Washington University
Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate.
Washington University
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.
Washington University
Design, Synthesis, and Characterization of 3-(Benzylidene)indolin-2-one Derivatives as Ligands fora-Synuclein Fibrils.
Washington University
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.
Washington University
Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.
Washington University
Synthesis, pharmacological evaluation and molecular modeling studies of triazole containing dopamine D3 receptor ligands.
Washington University
Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer.
Washington University
Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues ass2 receptor ligands.
Washington University
Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.
Washington University
Thes2 receptor: a novel protein for the imaging and treatment of cancer.
Washington University
Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter.
Washington University
Evaluation of N-phenyl homopiperazine analogs as potential dopamine D3 receptor selective ligands.
Washington University
Optimizing small molecule inhibitors of calcium-dependent protein kinase 1 to prevent infection by Toxoplasma gondii.
Washington University
Imaging reversal of multidrug resistance in living mice with bioluminescence: MDR1 P-glycoprotein transports coelenterazine.
Washington University
Exploring new near-infrared fluorescent disulfide-based cyclic RGD peptide analogs for potential integrin-targeted optical imaging.
Washington University
Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Washington University
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.
Washington University
Three-dimensional quantitative structure-activity relationship of human immunodeficiency virus (I) protease inhibitors. 2. Predictive power using limited exploration of alternate binding modes.
Washington University
Three-dimensional QSAR of human immunodeficiency virus (I) protease inhibitors. 1. A CoMFA study employing experimentally-determined alignment rules.
Washington University
Three-dimensional quantitative structure-activity relationship of angiotesin-converting enzyme and thermolysin inhibitors. II. A comparison of CoMFA models incorporating molecular orbital fields and desolvation free energies based on active-analog and complementary-receptor-field alignment rules.
Washington University
Synthesis, radiolabeling and initial in vivo evaluation of [(11)C]KSM-01 for imaging PPAR-a receptors.
Washington University
Near-infrared fluorescent divalent RGD ligand for integrinavß3-targeted optical imaging.
Washington University
Biotinylated quercetin as an intrinsic photoaffinity proteomics probe for the identification of quercetin target proteins.
Washington University
Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine.
Washington University
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
Washington University
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
Washington University
Novel bioactive and stable neurotensin peptide analogues capable of delivering radiopharmaceuticals and molecular beacons to tumors.
Washington University
Conformationally restricted TRH analogs: a probe for the pyroglutamate region.
Washington University
Novel cyclic analogs of angiotensin II with cyclization between positions 5 and 7: conformational and biological implications.
Washington University
Effects of steroid D-ring modification on suicide inactivation and competitive inhibition of aromatase by analogues of androsta-1,4-diene-3,17-dione.
Washington University
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues fors1 receptors.
Washington University
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
Washington University
Synthesis and characterization of selective dopamine D2 receptor ligands using aripiprazole as the lead compound.
Washington University
Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.
Washington University
Synthesis and pharmacological evaluation of fluorine-containing D3 dopamine receptor ligands.
Washington University
Rapid clinical induction of hepatic cytochrome P4502B6 activity by ritonavir.
Washington University
Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.
Washington University
Design and synthesis of 2-amino-4-methylpyridine analogues as inhibitors for inducible nitric oxide synthase and in vivo evaluation of [18F]6-(2-fluoropropyl)-4-methyl-pyridin-2-amine as a potential PET tracer for inducible nitric oxide synthase.
Washington University
New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.
Washington University
Modulating G-protein coupled receptor/G-protein signal transduction by small molecules suggested by virtual screening.
Washington University
Isatin sulfonamide analogs containing a Michael addition acceptor: a new class of caspase 3/7 inhibitors.
Washington University
Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography.
Washington University
Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis.
Washington University
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
Washington University
Synthesis, in vitro receptor binding, and in vivo evaluation of fluorescein and carbocyanine peptide-based optical contrast agents.
Washington University
Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.
Washington University
Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor.
Washington University
Thyrotropin releasing hormone analogs: a building block approach to the construction of tetracyclic peptidomimetics.
Washington University
Synthesis and evaluation of two positron-labeled nitric oxide synthase inhibitors, S-[11C]methylisothiourea and S-(2-[18F]fluoroethyl)isothiourea, as potential positron emission tomography tracers.
Washington University
Multiple binding modes for the receptor-bound conformations of cyclic AII agonists.
Washington University
Structural determinants of haloenol lactone-mediated suicide inhibition of canine myocardial calcium-independent phospholipase A2.
Washington University
Ac-[3- and 4-alkylthioproline31]-CCK4 analogs: synthesis and implications for the CCK-B receptor-bound conformation.
Washington University
N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.
Washington University
Trifluoromethylacetylenic alcohols as affinity labels: inactivation of estradiol dehydrogenase by a trifluoromethylacetylenic secostradiol.
Washington University
Substituted benzimidazoles, their preparation and their use as pharmaceuticals
Neomed Institute
Compositions and methods for the production of pyrimidine and pyridine compounds with BTK inhibitory activity
Merck Patent
Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ROR[γ]
Phenex Pharmaceuticals
Synthesis and biological activity of derivatives of tetrahydroacridine as acetylcholinesterase inhibitors.
Medical University of Lodz