141 articles for thisTarget
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Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
Uppsala University
Kinetically Selective Inhibitors of Human Carbonic Anhydrase Isozymes I, II, VII, IX, XII, and XIII.
Uppsala University
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.
Uppsala University
Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.
Uppsala University
3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1.
Uppsala University
N-Substituted pyrazole-3-carboxamides as inhibitors of human 15-lipoxygenase.
Uppsala University
Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands.
Uppsala University
Exploration and pharmacokinetic profiling of phenylalanine based carbamates as novel substance p 1-7 analogues.
Uppsala University
Synthesis and evaluation of isoleucine derived angiotensin II AT(2) receptor ligands.
Uppsala University
DXR inhibition by potent mono- and disubstituted fosmidomycin analogues.
Uppsala University
Constrained H-Phe-Phe-NH2 analogues with high affinity to the substance P 1-7 binding site and with improved metabolic stability and cell permeability.
Uppsala University
Novel pseudopeptides incorporating a benzodiazepine-based turn mimetic--targeting Mycobacterium tuberculosis ribonucleotide reductase.
Uppsala University
Synthesis and pharmacology of the enantiomers of cis-7-hydroxy-3-methyl-2-(dipropylamino)tetralin.
Uppsala University
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Uppsala University
Selective angiotensin II AT(2) receptor agonists with reduced CYP 450 inhibition.
Uppsala University
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
Uppsala University
Two new isoflavones from Ceiba pentandra and their effect on cyclooxygenase-catalyzed prostaglandin biosynthesis.
Uppsala University
Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis.
Uppsala University
Structures of Mycobacterium tuberculosis 1-deoxy-D-xylulose-5-phosphate reductoisomerase provide new insights into catalysis.
Uppsala University
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.
Uppsala University
Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors.
Uppsala University
Synthesis of a new class of druglike angiotensin II C-terminal mimics with affinity for the AT2 receptor.
Uppsala University
Design, synthesis, and incorporation of a beta-turn mimetic in angiotensin II forming novel pseudopeptides with affinity for AT1 and AT2 receptors.
Uppsala University
Microwave-accelerated synthesis of P1'-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold.
Uppsala University
Angiotensin II pseudopeptides containing 1,3,5-trisubstituted benzene scaffolds with high AT2 receptor affinity.
Uppsala University
New selective AT2 receptor ligands encompassing a gamma-turn mimetic replacing the amino acid residues 4-5 of angiotensin II act as agonists.
Uppsala University
AT2-selective angiotensin II analogues containing tyrosine-functionalized 5,5-bicyclic thiazabicycloalkane dipeptide mimetics.
Uppsala University
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.
Uppsala University
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Uppsala University
A selective AT2 receptor ligand with a gamma-turn-like mimetic replacing the amino acid residues 4-5 of angiotensin II.
Uppsala University
Design and synthesis of dihydrofolate reductase inhibitors encompassing a bridging ester group. Evaluation in a mouse colitis model.
Uppsala University
Vinyl sulfide cyclized analogues of angiotensin II with high affinity and full agonist activity at the AT(1) receptor.
Uppsala University
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Uppsala University
Computational predictions of binding affinities to dihydrofolate reductase: synthesis and biological evaluation of methotrexate analogues.
Uppsala University
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.
Uppsala University
trans-2-Aryl-N,N-dipropylcyclopropylamines: synthesis and interactions with 5-HT(1A) receptors.
Uppsala University
Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors.
Uppsala University
A 3-D model for 5-HT1A-receptor agonists based on stereoselective methyl-substituted and conformationally restricted analogues of 8-hydroxy-2-(dipropylamino)tetralin.
Uppsala University
N-alkylaminoacids and their derivatives interact with melanocortin receptors.
Uppsala University
Inhibition of hepatitis C virus NS3 protease activity by product-based peptides is dependent on helicase domain.
Uppsala University
Substitution of the phosphonic acid and hydroxamic acid functionalities of the DXR inhibitor FR900098: an attempt to improve the activity against Mycobacterium tuberculosis.
Uppsala University
Potent macrocyclic inhibitors of insulin-regulated aminopeptidase (IRAP) by olefin ring-closing metathesis.
Uppsala University
Investigation ofa-phenylnorstatine anda-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors.
Uppsala University
Disulfide cyclized tripeptide analogues of angiotensin IV as potent and selective inhibitors of insulin-regulated aminopeptidase (IRAP).
Uppsala University
Discovery of dipeptides with high affinity to the specific binding site for substance P1-7.
Uppsala University
alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases.
Uppsala University
Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.
Uppsala University
Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships.
Uppsala University
Ligands to the (IRAP)/AT4 receptor encompassing a 4-hydroxydiphenylmethane scaffold replacing Tyr2.
Uppsala University
Identification of MMP-12 inhibitors by using biosensor-based screening of a fragment library.
Uppsala University
Evaluation of the amino acid binding site of Mycobacterium tuberculosis glutamine synthetase for drug discovery.
Uppsala University
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
Uppsala University
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
Uppsala University
Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay.
Uppsala University
Cox-2 inhibitory effects of naturally occurring and modified fatty acids.
Uppsala University
Selective angiotensin II AT(2) receptor agonists devoid of the imidazole ring system.
Uppsala University
Design and synthesis of a library of tertiary amides: evaluation as mimetics of the melanocortins' active core.
Uppsala University
Structure-based virtual screening discovers potent and selective adenosine A
Uppsala University
α-Aminophosphonate inhibitors of metallo-β-lactamases NDM-1 and VIM-2.
Uppsala University
Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships.
Uppsala University
2-Alkyl substituted benzimidazoles as a new class of selective AT2 receptor ligands.
Uppsala University
A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold.
Uppsala University
Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations.
Uppsala University
Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor.
Uppsala University
Importance of Binding Site Hydration and Flexibility Revealed When Optimizing a Macrocyclic Inhibitor of the Keap1-Nrf2 Protein-Protein Interaction.
Uppsala University
New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of"THIQ".
Uppsala University
Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.
Uppsala University
Spatial Distribution and Stability of Cholinesterase Inhibitory Protoberberine Alkaloids from
Uppsala University
Functional Characterization of the Nemertide α Family of Peptide Toxins.
Uppsala University
First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo.
Uppsala University
Macrocyclic peptidomimetics as inhibitors of insulin-regulated aminopeptidase (IRAP).
Uppsala University
Reductive amination products containing naphthalene and indole moieties bind to melanocortin receptors.
Uppsala University
N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.
Uppsala University
Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii.
Uppsala University
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A
Uppsala University
Atropisomeric derivatives of 2',6'-disubstituted (R)-11-phenylaporphine: selective serotonin 5-HT(7) receptor antagonists.
Uppsala University
Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives.
Uppsala University
Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.
Uppsala University
Inhibitors of the C(2)-symmetric HIV-1 protease: nonsymmetric binding of a symmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains.
Uppsala University
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
Uppsala University
Novel derivatives of 3-(dipropylamino)chroman. Interactions with 5-HT1A and D2A receptors.
Uppsala University
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
Uppsala University
11-substituted (R)-aporphines: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions.
Uppsala University
10-substituted 11-oxygenated (R)-aporphines: synthesis, pharmacology, and modeling of 5-HT1A receptor interactions.
Uppsala University
Design, synthesis and in vitro biological evaluation of oligopeptides targeting E. coli type I signal peptidase (LepB).
Uppsala University
Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket.
Uppsala University
Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2-P1' Region.
Uppsala University
Design and synthesis of P1-P3 macrocyclic tertiary-alcohol-comprising HIV-1 protease inhibitors.
Uppsala University
(R)-11-hydroxy- and (R)-11-hydroxy-10-methylaporphine: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions.
Uppsala University
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.
Uppsala University
Derivatives of cis-2-amino-8-hydroxy-1-methyltetralin: mixed 5-HT1A-receptor agonists and dopamine D2-receptor antagonists.
Uppsala University
Derivatives of 2-(dipropylamino)tetralin: effect of the C8-substituent on the interaction with 5-HT1A receptors.
Uppsala University
Synthesis, X-ray analysis, and biological evaluation of a new class of stereopure lactam-based HIV-1 protease inhibitors.
Uppsala University
Discovery of achiral inhibitors of the hepatitis C virus NS3 protease based on 2(1H)-pyrazinones.
Uppsala University
Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents.
Uppsala University
Proteochemometrics mapping of the interaction space for retroviral proteases and their substrates.
Uppsala University
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.
Uppsala University
Combining docking, molecular dynamics and the linear interaction energy method to predict binding modes and affinities for non-nucleoside inhibitors to HIV-1 reverse transcriptase.
Uppsala University
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.
Uppsala University
Additional level of information about complex interaction between non-nucleoside inhibitor and HIV-1 reverse transcriptase using biosensor-based thermodynamic analysis.
Uppsala University
Cyclodextrin-derived diorganyl tellurides as glutathione peroxidase mimics and inhibitors of thioredoxin reductase and cancer cell growth.
Uppsala University
QSAR and proteo-chemometric analysis of the interaction of a series of organic compounds with melanocortin receptor subtypes.
Uppsala University
Angiotensin II analogues encompassing 5,9- and 5,10-fused thiazabicycloalkane tripeptide mimetics.
Uppsala University
Design, synthesis, and biological activities of four angiotensin II receptor ligands with gamma-turn mimetics replacing amino acid residues 3-5.
Uppsala University
Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.
Uppsala University
3-(2-Benzofuranyl)quinuclidin-2-ene derivatives: novel muscarinic antagonists.
Uppsala University
Boronic ester-linked macrocyclic lipopeptides as serine protease inhibitors targeting Escherichia coli type I signal peptidase.
Uppsala University
Docking Screens for Dual Inhibitors of Disparate Drug Targets for Parkinson's Disease.
Uppsala University
Analogues of the muscarinic agent 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane]: synthesis and pharmacology.
Uppsala University
Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
Amgen
Neoflavonoids and Tetrahydroquinolones as Possible Cancer Chemopreventive Agents.
Central Institute of Medicinal and Aromatic Plants
Characterization of human alpha 4 beta 2-nicotinic acetylcholine receptors stably and heterologously expressed in native nicotinic receptor-null SH-EP1 human epithelial cells.
Barrow Neurological Institute
Amide compounds for treatment of complement mediated disorders
Achillion Pharmaceuticals
Design, parallel synthesis, and crystal structures of biphenyl antithrombotics as selective inhibitors of tissue factor FVIIa complex. Part 1: Exploration of S2 pocket pharmacophores.
Biocryst Pharmaceuticals
Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking.
H. Lee Moffitt Cancer Center