109 articles for thisTarget
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An epigenetic modifier induces production of (10'S)-verruculide B, an inhibitor of protein tyrosine phosphatases by Phoma sp. nov. LG0217, a fungal endophyte of Parkinsonia microphylla.
University of Arizona
Oxaspirol B with p97 Inhibitory Activity and Other Oxaspirols from Lecythophora sp. FL1375 and FL1031, Endolichenic Fungi Inhabiting Parmotrema tinctorum and Cladonia evansii.
University of Arizona
Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligands.
University of Arizona
Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives.
University of Arizona
Design, synthesis and biological evaluation of multifunctional ligands targeting opioid and bradykinin 2 receptors.
University of Arizona
Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.
University of Arizona
Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.
University of Arizona
Discovery of Potent 17ß-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.
University of Arizona
Development of a time-resolved fluorescence probe for evaluation of competitive binding to the cholecystokinin 2 receptor.
University of Arizona
Synthesis and evaluation of bivalent ligands for binding to the human melanocortin-4 receptor.
University of Arizona
Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.
University of Arizona
Interaction of 2,3-dimercapto-1-propane sulfonate with the human organic anion transporter hOAT1.
University of Arizona
Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1.
University of Arizona
Interaction of cysteine conjugates with human and rabbit organic anion transporter 1.
University of Arizona
Development of potent µ and d opioid agonists with high lipophilicity.
University of Arizona
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
University of Arizona
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
University of Arizona
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
University of Arizona
Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: discovery of potent and selective hMC5R receptor antagonists.
University of Arizona
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
University of Arizona
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
University of Arizona
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
University of Arizona
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.
University of Arizona
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
University of Arizona
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University of Arizona
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
University of Arizona
Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors.
University of Arizona
Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors.
University of Arizona
A new approach to search for the bioactive conformation of glucagon: positional cyclization scanning.
University of Arizona
Design and synthesis of conformationally constrained glucagon analogues.
University of Arizona
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
University of Arizona
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.
University of Arizona
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
University of Arizona
The role of phenylalanine at position 6 in glucagon's mechanism of biological action: multiple replacement analogues of glucagon.
University of Arizona
The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid recepto
University of Arizona
Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences.
University of Arizona
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
University of Arizona
Newly discovered stereochemical requirements in the side-chain conformation of delta opioid agonists for recognizing opioid delta receptors.
University of Arizona
[L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity.
University of Arizona
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
University of Arizona
[D-Pen2,D-Pen5]enkephalin analogues with increased affinity and selectivity for delta opioid receptors.
University of Arizona
Synthesis of highly mu and delta opioid receptor selective peptides containing a photoaffinity group.
University of Arizona
Selection of cyclic-peptide inhibitors targeting Aurora kinase A: problems and solutions.
University of Arizona
Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.
University of Arizona
Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG).
University of Arizona
Cyclic lactam hybrida-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
University of Arizona
Discovery of a potent and efficacious peptide derivative ford/µ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
University of Arizona
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
University of Arizona
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
University of Arizona
Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain.
University of Arizona
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
University of Arizona
Catalytic inhibition of topoisomerase IIalpha by demethylzeylasterone, a 6-oxophenolic triterpenoid from Kokoona zeylanica.
University of Arizona
Synthesis, Optimization, and Structure-Activity Relationships of Nicotinamide Phosphoribosyltransferase (NAMPT) Positive Allosteric Modulators (N-PAMs).
University of Arizona
Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors.
University of Arizona
Discovery and Development of a Selective Inhibitor of the ER Resident Chaperone Grp78.
University of Arizona
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
University of Arizona
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
University of Arizona
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
University of Arizona
Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.
University of Arizona
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
University of Arizona
Synthesis and biological activity of the first cyclic biphalin analogues.
University of Arizona
New PDMP analogues inhibit process outgrowth in an insect cell line.
University of Arizona
Novel targeting strategy based on multimeric ligands for drug delivery and molecular imaging: homooligomers of alpha-MSH.
University of Arizona
Structure-activity relationships of gamma-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. Discovery of highly selective hMC3R, hMC4R, and hMC5R analogues.
University of Arizona
Design of novel chimeric melanotropin-deltorphin analogues. Discovery of the first potent human melanocortin 1 receptor antagonist.
University of Arizona
Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.
University of Arizona
Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.
University of Arizona
A high throughput substrate binding assay reveals hexachlorophene as an inhibitor of the ER-resident HSP70 chaperone GRP78.
University of Arizona
Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.
University of Arizona
Novel CDC25A phosphatase inhibitors from pyrolysis of 3-alpha-azido-B-homo-6-oxa-4-cholesten-7-one on silica gel.
University of Arizona
Discovery of a novel series of potent and selective substrate-based inhibitors of p60c-src protein tyrosine kinase: conformational and topographical constraints in peptide design.
University of Arizona
Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
University of Arizona
Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
University of Arizona
Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations.
University of Arizona
Discovery of Novel Multifunctional Ligands with μ/δ Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.
University of Arizona
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.
University of Arizona
Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
University of Arizona
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
University of Arizona
Synthesis and biological evaluation of novobiocin analogues as potential heat shock protein 90 inhibitors.
University of Arizona
Synthesis and characterization of time-resolved fluorescence probes for evaluation of competitive binding to melanocortin receptors.
University of Arizona
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
University of Arizona
Highly kappa receptor-selective dynorphin A analogues with modifications in position 3 of dynorphin A(1-11)-NH2.
University of Arizona
Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
University of Arizona
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
University of Arizona
Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
University of Arizona
Design and synthesis of somatostatin analogues with topographical properties that lead to highly potent and specific mu opioid receptor antagonists with greatly reduced binding at somatostatin receptors.
University of Arizona
Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors.
University of Arizona
Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
University of Arizona
ATP-competitive, marine derived natural products that target the DEAD box helicase, eIF4A.
University of Arizona
Ring substituted and other conformationally constrained tyrosine analogues of [D-Pen2,D-Pen5]enkephalin with delta opioid receptor selectivity.
University of Arizona
Naphthyridine compounds, medical combinations and use thereof
Nanjing Natinefy Pharmatech
Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface.
Smithkline Beecham Pharmaceuticals
Synthesis and SAR studies of indole-based MK2 inhibitors.
Boehringer Ingelheim Pharmaceuticals
Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP).
University of Michigan
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
Universita Degli Studi Di Firenze