82 articles for thisTarget
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Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.
University of Kansas
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites.
University of Kansas
Identification of a Small Molecule Cyclophilin D Inhibitor for Rescuing Aß-Mediated Mitochondrial Dysfunction.
University of Kansas
Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity.
University of Kansas
Evaluation of inhibition selectivity for human cytochrome P450 2A enzymes.
University of Kansas
Human Toll-like receptor 8-selective agonistic activities in 1-alkyl-1H-benzimidazol-2-amines.
University of Kansas
Expanding the results of a high throughput screen against an isochorismate-pyruvate lyase to enzymes of a similar scaffold or mechanism.
University of Kansas
Chiral DNA gyrase inhibitors. 3. Probing the chiral preference of the active site of DNA gyrase. Synthesis of 10-fluoro-6-methyl-6,7-dihydro-9-piperazinyl- 2H-benzo[a]quinolizin-20-one-3-carboxylic acid analogues.
University of Kansas
Identification of human presequence protease (hPreP) agonists for the treatment of Alzheimer's disease.
University of Kansas
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
University of Kansas
Novel endotoxin-sequestering compounds with terephthalaldehyde-bis-guanylhydrazone scaffolds.
University of Kansas
9-(trans-2',trans-3'-dihydroxycyclopent-4'-enyl) derivatives of adenine and 3-deazaadenine: potent inhibitors of bovine liver S-adenosylhomocysteine hydrolase.
University of Kansas
Structure-activity relationships in human Toll-like receptor 8-active 2,3-diamino-furo[2,3-c]pyridines.
University of Kansas
Structure-activity relationships in human Toll-like receptor 2-specific monoacyl lipopeptides.
University of Kansas
Toll-like receptor (TLR)-7 and -8 modulatory activities of dimeric imidazoquinolines.
University of Kansas
A docking score function for estimating ligand-protein interactions: application to acetylcholinesterase inhibition.
University of Kansas
Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and the alpha2-adrenoceptor.
University of Kansas
Adenosine-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase.
University of Kansas
Conformationally restricted and conformationally defined tyramine analogues as inhibitors of phenylethanolamine N-methyltransferase.
University of Kansas
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 11. Molecular dissections of neplanocin A as potential inhibitors of S-adenosylhomocysteine hydrolase.
University of Kansas
Linear free energy relationship studies of enzyme active site binding: thymidylate synthase.
University of Kansas
Conformational and steric aspects of the inhibition of phenylethanolamine N-methyltransferase by benzylamines.
University of Kansas
Stereochemical aspects of phenylethanolamine analogues as substrates of phenylethanolamine N-methyltransferase.
University of Kansas
Inhibition of phenylethanolamine N-methyltransferase (PNMT) by aromatic hydroxy-substituted 1,2,3,4,-tetrahydroisoquinolines: further studies on the hydrophilic pocket of the aromatic ring binding region of the active site.
University of Kansas
Binding orientation of amphetamine and norfenfluramine analogues in the benzonorbornene and benzobicyclo[3.2.1]octane ring systems at the active site of phenylethanolamine N-methyltransferase (PNMT)
University of Kansas
Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme.
University of Kansas
Structure-activity relationships in toll-like receptor 2-agonists leading to simplified monoacyl lipopeptides.
University of Kansas
Preliminary evaluation of a 3H imidazoquinoline library as dual TLR7/TLR8 antagonists.
University of Kansas
Toward self-adjuvanting subunit vaccines: model peptide and protein antigens incorporating covalently bound toll-like receptor-7 agonistic imidazoquinolines.
University of Kansas
Structure-activity relationships in nucleotide oligomerization domain 1 (Nod1) agonistic¿-glutamyldiaminopimelic acid derivatives.
University of Kansas
Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7.
University of Kansas
Structure-activity relationships in human toll-like receptor 7-active imidazoquinoline analogues.
University of Kansas
Structure-activity relationships in toll-like receptor-2 agonistic diacylthioglycerol lipopeptides.
University of Kansas
The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
University of Kansas
Regioisomerism-dependent TLR7 agonism and antagonism in an imidazoquinoline.
University of Kansas
Inhibition of monometalated methionine aminopeptidase: inhibitor discovery and crystallographic analysis.
University of Kansas
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.
University of Kansas
Design, synthesis, and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues.
University of Kansas
Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis.
University of Kansas
Application of the Goldilocks effect to the design of potent and selective inhibitors of phenylethanolamine N-methyltransferase: balancing pKa and steric effects in the optimization of 3-methyl-1,2,3,4-tetrahydroisoquinoline inhibitors by beta-fluorination.
University of Kansas
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.
University of Kansas
Nanomolar inhibitors of CNS epinephrine biosynthesis: (R)-(+)-3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines as potent and highly selective inhibitors of phenylethanolamine N-methyltransferase1.
University of Kansas
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.
University of Kansas
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.
University of Kansas
Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity toward the alpha2-adrenoceptor.
University of Kansas
Design of Transmembrane Mimetic Structural Probes to Trap Different Stages of γ-Secretase-Substrate Interaction.
University of Kansas
Identification of a Human Toll-Like Receptor (TLR) 8-Specific Agonist and a Functional Pan-TLR Inhibitor in 2-Aminoimidazoles.
University of Kansas
Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine
University of Kansas
Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
University of Kansas
Further exploration of the structure-activity relationship of imidazoquinolines; identification of potent C7-substituted imidazoquinolines.
University of Kansas
Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
University of Kansas
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
University of Kansas
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
University of Kansas
3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.
University of Kansas
Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor.
University of Kansas
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
University of Kansas
Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
University of Kansas
Aristeromycin-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase.
University of Kansas
Potential Drug Abuse Therapeutics Derived from the Hallucinogenic Natural Product Salvinorin A.
University of Kansas
Natural products as tools for neuroscience: discovery and development of novel agents to treat drug abuse.
University of Kansas
Inactivation of thymidylate synthase at an alternate high-affinity binding site.
University of Kansas
Synthesis and evaluation of 3-substituted analogues of 1,2,3,4-tetrahydroisoquinoline as inhibitors of phenylethanolamine N-methyltransferase.
University of Kansas
Conformational preference for the binding of biaryl substrates and inhibitors to the active site of phenylethanolamine N-methyltransferase.
University of Kansas
Conformational requirements of substrates for activity with phenylethanolamine N-methyltransferase.
University of Kansas
Structure-Based Design of Inhibitors with Improved Selectivity for Steroidogenic Cytochrome P450 17A1 over Cytochrome P450 21A2.
University of Kansas
Design, synthesis, and opioid activity of arodyn analogs cyclized by ring-closing metathesis involving Tyr(allyl).
University of Kansas
Oxidation of neplanocin A to the corresponding 3'-keto derivative by S-adenosylhomocysteine hydrolase.
University of Kansas
4'-modified analogues of aristeromycin and neplanocin A: synthesis and inhibitory activity toward S-adenosyl-L-homocysteine hydrolase.
University of Kansas
Cannabidiol derivatives as inhibitors of the HIF prolyl hydroxylases activity
Emerald Health Pharmaceuticals
Carbazole and tetrahydrocarbazole compounds useful as inhibitors of BTK
Bristol-Myers Squibb
Structural basis of mycobacterial inhibition by cyclomarin A
Novartis Institute For Tropical Diseases
Antioxidant and acetylcholinesterase inhibition properties of novel bromophenol derivatives.
Ataturk University
Host properties of cyclodextrins towards anion constituents of antigenic determinants. A thermodynamic study in water and in N,N-dimethylformamide
University of Surrey