55 articles for thisTarget
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Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.
University of Bath
Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases.
University of Bath
Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.
University of Bath
Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases.
University of Bath
C7ß-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.
University of Bath
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
University of Bath
Cyclic adenosine 5'-diphosphate ribose analogs without a"southern" ribose inhibit ADP-ribosyl cyclase-hydrolase CD38.
University of Bath
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.
University of Bath
Structure-activity relationship of adenosine 5'-diphosphoribose at the transient receptor potential melastatin 2 (TRPM2) channel: rational design of antagonists.
University of Bath
Design and Discovery of 2-Arylquinazolin-4-ones as Potent and Selective Inhibitors of Tankyrases.
University of Bath
One-pot tandem Hurtley-retro-Claisen-cyclisation reactions in the synthesis of 3-substituted analogues of 5-aminoisoquinolin-1-one (5-AIQ), a water-soluble inhibitor of PARPs.
University of Bath
Adamantyl carboxamides and acetamides as potent human 11ß-hydroxysteroid dehydrogenase type 1 inhibitors.
University of Bath
Contribution of phosphates and adenine to the potency of adenophostins at the IP3 receptor: synthesis of all possible bisphosphates of adenophostin A.
University of Bath
Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors.
University of Bath
Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
University of Bath
14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
University of Bath
Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design.
University of Bath
Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents.
University of Bath
Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
University of Bath
Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.
University of Bath
Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.
University of Bath
E-ring modified steroids as novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.
University of Bath
Novel and potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors.
University of Bath
Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
University of Bath
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
University of Bath
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.
University of Bath
The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.
University of Bath
Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
University of Bath
Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165.
University of Bath
Synthesis and biological activity of the superestrogen (E)-17-oximino-3-O-sulfamoyl-1,3,5(10)-estratriene: x-ray crystal structure of (E)-17-oximino-3-hydroxy-1,3,5(10)-estratriene.
University of Bath
Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates.
University of Bath
Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential.
University of Bath
2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents.
University of Bath
Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II.
University of Bath
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
University of Bath
5-Benzamidoisoquinolin-1-ones and 5-(κ-carboxyalkyl)isoquinolin-1-ones as isoform-selective inhibitors of poly(ADP-ribose) polymerase 2 (PARP-2).
University of Bath
Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
University of Bath
3,17-disubstituted 2-alkylestra-1,3,5(10)-trien-3-ol derivatives: synthesis, in vitro and in vivo anticancer activity.
University of Bath
2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity.
University of Bath
A-ring-substituted estrogen-3-O-sulfamates: potent multitargeted anticancer agents.
University of Bath
A novel 18 beta-glycyrrhetinic acid analogue as a potent and selective inhibitor of 11 beta-hydroxysteroid dehydrogenase 2.
University of Bath
Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin-Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme.
University of Bath
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.
University of Bath
Synthesis, calcium mobilizing, and physicochemical properties of D-chiro-inositol 1,3,4,6-tetrakisphosphate, a novel and potent ligand at the D-myo-inositol 1,4,5-trisphosphate receptor.
University of Bath
Molecular Basis for Multiple Omapatrilat Binding Sites within the ACE C-Domain: Implications for Drug Design.
University of Bath
The synthesis and kinetic evaluation of aryl α-aminophosphonates as novel inhibitors of T. cruzi trans-sialidase.
University of Bath
Pyrrolidine-2, 5-dione derivatives, pharmaceutical compositions and methods for use as IDO1 inhibitors
Iteos Therapeutics
5,6-Dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase.
Anadys Pharmaceuticals
Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication.
Schering-Plough Research Institute