54 articles for thisTarget
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Pharmacophore Mapping of Thienopyrimidine-Based Monophosphonate (ThP-MP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase.
Mcgill University
Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidin
Mcgill University
3-Oxo-hexahydro-1H-isoindole-4-carboxylic Acid as a Drug Chiral Bicyclic Scaffold: Structure-Based Design and Preparation of Conformationally Constrained Covalent and Noncovalent Prolyl Oligopeptidase Inhibitors.
Mcgill University
Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase.
Mcgill University
Modular assembly of purine-like bisphosphonates as inhibitors of HIV-1 reverse transcriptase.
Mcgill University
Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: implications to drug discovery for neurodegenerative diseases.
Mcgill University
Shuttle-cargo fusion molecules of transport peptides and the hD2/3 receptor antagonist fallypride: a feasible approach to preserve ligand-receptor binding?
Mcgill University
Inhibition of 5-oxo-6,8,11,14-eicosatetraenoic acid-induced activation of neutrophils and eosinophils by novel indole OXE receptor antagonists.
Mcgill University
Thienopyrimidine bisphosphonate (ThPBP) inhibitors of the human farnesyl pyrophosphate synthase: optimization and characterization of the mode of inhibition.
Mcgill University
Discovery of thienopyrimidine-based inhibitors of the human farnesyl pyrophosphate synthase--parallel synthesis of analogs via a trimethylsilyl ylidene intermediate.
Mcgill University
Design of potent bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase via targeted interactions with the active site 'capping' phenyls.
Mcgill University
Virtual screening and computational optimization for the discovery of covalent prolyl oligopeptidase inhibitors with activity in human cells.
Mcgill University
Design and synthesis of active site inhibitors of the human farnesyl pyrophosphate synthase: apoptosis and inhibition of ERK phosphorylation in multiple myeloma cells.
Mcgill University
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
Mcgill University
Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.
Mcgill University
Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.
Mcgill University
Synthesis and structure-activity relationships of truncated bisubstrate inhibitors of aminoglycoside 6'-N-acetyltransferases.
Mcgill University
An o-aminoanilide analogue of 1a,25-dihydroxyvitamin D(3) functions as a strong vitamin D receptor antagonist.
Mcgill University
Mechanism of hepatitis C virus RNA polymerase inhibition with dihydroxypyrimidines.
Mcgill University
Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase.
Mcgill University
Constrained peptidomimetics reveal detailed geometric requirements of covalent prolyl oligopeptidase inhibitors.
Mcgill University
Structure-Activity Relationship of Inositol Thiophosphate Analogs as Allosteric Activators of Clostridioides difficile Toxin B.
McGill University
Design, synthesis and antiproliferative activity of raloxifene/histone deacetylase inhibitor hybrids in breast cancer.
McGill University
Discovery and Evaluation of C6-Substituted Pyrazolopyrimidine-Based Bisphosphonate Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase and Evaluation of Their Antitumor Efficacy in Multiple Myeloma, Pancreatic Ductal Adenocarcinoma, and Colorectal Cancer.
Mcgill University
Discovery, Synthesis, and In Vitro Characterization of 2,3 Derivatives of 4,5,6,7-Tetrahydro-Benzothiophene as Potent Modulators of Retinoic Acid Receptor-Related Orphan Receptor γt.
Mcgill University
Novel Aurora A and Protein Kinase C (α, β1, β2, and θ) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.
Mcgill University
Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.
Mcgill University
Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat.
Mcgill University
Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase.
Mcgill University
Unraveling the Prenylation-Cancer Paradox in Multiple Myeloma with Novel Geranylgeranyl Pyrophosphate Synthase (GGPPS) Inhibitors.
Mcgill University
Chirality-Driven Mode of Binding of α-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS).
Mcgill University
Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α.
Mcgill University
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
Mcgill University
Functional characterization of IRESes by an inhibitor of the RNA helicase eIF4A.
Mcgill University
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.
Mcgill University
Pyrophosphorolytic excision of nonobligate chain terminators by hepatitis C virus NS5B polymerase.
Mcgill University
The pyrophosphate analogue foscarnet traps the pre-translocational state of HIV-1 reverse transcriptase in a Brownian ratchet model of polymerase translocation.
Mcgill University
Probing the ligand preferences of the three types of bacterial pantothenate kinase.
Mcgill University
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
Mcgill University
Pharmacophore requirements for HIV-1 reverse transcriptase inhibitors that selectively "Freeze" the pre-translocated complex during the polymerization catalytic cycle.
Mcgill University
Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
Wisconsin Alumni Research Foundation
Use of inhibitor of apoptosis protein (IAP) antagonists in HIV therapy
Sanford Burnham Prebys Medical Discovery Institute
9-(pyrazol-3-yl)-9H-purine-2-amine and 3-(pyrazol-3-yl) -3H-imidazo[4,5-B] pyridin-5-amine derivatives and their use for the treatment of cancer
Astrazeneca
Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc.
Chemical Genomics Centre of The Max Planck Society