PMID

Data

Article Title

Organization

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

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

Design and discovery of boronic acid drugs.

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

Periodinates: a new class of protein tyrosine phosphatase 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

Discovery of covalent prolyl oligopeptidase boronic ester inhibitors.

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

Imidazole derivatives as formyl peptide receptor modulators

Allergan

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

A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells.

Virginia Commonwealth University