J. Falgueyret

发表

Identification and localization of 7B2 protein in human, porcine, and rat thyroid gland and in human medullary carcinoma.

N. Seidah, M. Marcinkiewicz, S. Benjannet, 1988, Endocrinology.

Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.

J. R. Somoza, Dan Wang, J. Falgueyret, 2005, Journal of medicinal chemistry.

Reconstitution of a 10-gene pathway for synthesis of the plant alkaloid dihydrosanguinarine in Saccharomyces cerevisiae

V. Martin, E. Fossati, J. Falgueyret, 2014, Nature Communications.

Synthesis of Morphinan Alkaloids in Saccharomyces cerevisiae

V. Martin, E. Fossati, J. Falgueyret, 2015, PloS one.

Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.

Sébastien Gagné, Eric Langlois, Jean-François Truchon, 2014, Bioorganic & medicinal chemistry letters.

Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase.

J. Falgueyret, S. Charleson, J. Evans, 1995, Journal of medicinal chemistry.

The discovery and synthesis of potent zwitterionic inhibitors of renin.

J. Falgueyret, M. Percival, S. Gagné, 2011, Bioorganic & medicinal chemistry letters.

A High-Throughput Continuous Assay for Screening and Characterization of Inhibitors of HIV Reverse-Transcriptase DNA Polymerase Activity

J. Falgueyret, R. Melnyk, E. Cauchon, 2011, Journal of biomolecular screening.

An activity-based probe for the determination of cysteine cathepsin protease activities in whole cells.

J. Falgueyret, S. Venkatraman, M. Percival, 2004, Analytical biochemistry.

Characterization of the arachidonate and ATP binding sites of human 5-lipoxygenase using photoaffinity labeling and enzyme immobilization.

J. Falgueyret, D. Riendeau, J. Hutchinson, 1995, Biochemistry.

In Vitro Characterization of MK-1439, a Novel HIV-1 Nonnucleoside Reverse Transcriptase Inhibitor

Jason Burch, Yves Ducharme, Louis-Charles Campeau, 2013, Antimicrobial Agents and Chemotherapy.

A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.

J. Falgueyret, J. Palmer, C. Bryant, 2003, Journal of medicinal chemistry.

Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.

J. Falgueyret, R. Rydzewski, M. Percival, 2001, Journal of medicinal chemistry.

Chromogranin B (secretogranin I), a putative precursor of two novel pituitary peptides through processing at paired basic residues

M. Marcinkiewicz, S. Benjannet, J. Falgueyret, 1987, FEBS letters.

LTA4-derived 5-oxo-eicosatetraenoic acid: pH-dependent formation and interaction with the LTB4 receptor of human polymorphonuclear leukocytes

J. Falgueyret, D. Riendeau, 2000 .

LTA(4)-derived 5-oxo-eicosatetraenoic acid: pH-dependent formation and interaction with the LTB(4) receptor of human polymorphonuclear leukocytes.

J. Falgueyret, D. Riendeau, 2000, Biochimica et Biophysica Acta.

Identification of 5-keto-(7E,9E,11Z,14Z)-eicosatetraenoic acid as a novel nonenzymatic rearrangement product of leukotriene A4.

J. Falgueyret, D. Riendeau, J. Yergey, 1993, Archives of biochemistry and biophysics.

Adenovirus IL-13-induced airway disease in mice: a corticosteroid-resistant model of severe asthma.

Christopher M. Tan, D. Slipetz, H. Houshyar, 2008, American journal of respiratory cell and molecular biology.

3,4-Diarylpiperidines as potent renin inhibitors.

J. Falgueyret, Yongxin Han, E. Cauchon, 2012, Bioorganic & medicinal chemistry letters.

Justicidin E: A new leukotriene biosynthesis inhibitor.

J. Falgueyret, D. Riendeau, J. Guay, 1993 .

Inhibition of human leukocyte 5-lipoxygenase by a 4-hydroxybenzofuran, L-656,224. Evidence for enzyme reduction and inhibitor degradation.

J. Falgueyret, D. Riendeau, C. Rouzer, 1991, Biochemical pharmacology.

Pseudoperoxidase activity of 5-lipoxygenase stimulated by potent benzofuranol and N-hydroxyurea inhibitors of the lipoxygenase reaction.

J. Falgueyret, D. Riendeau, S. Yamamoto, 1991, The Biochemical journal.

Selective inhibitors of COX-2.

J. Falgueyret, B. Kennedy, C. Chan, 1995, Agents and actions. Supplements.

Criteria for the identification of non-redox inhibitors of 5-lipoxygenase.

J. Falgueyret, D. Riendeau, J. Hutchinson, 1993, Biochemical pharmacology.

Catalytic Properties and Reaction Mechanism of 5-Lipoxygenase

J. Falgueyret, M. Percival, D. Riendeau, 1991 .

Interfacial catalysis and production of a high ratio of leukotriene A4 to 5-HPETE by 5-lipoxygenase in a coupled assay with phospholipase A2.

J. Falgueyret, D. Riendeau, I. Street, 1993, Journal of lipid mediators.

Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein.

J. Falgueyret, D. Riendeau, R. Young, 2008, Bioorganic & medicinal chemistry letters.

Impact of Primer-induced Conformational Dynamics of HIV-1 Reverse Transcriptase on Polymerase Translocation and Inhibition*

J. Falgueyret, G. Beilhartz, R. Melnyk, 2011, The Journal of Biological Chemistry.

Probing cathepsin S activity in whole blood by the activity-based probe BIL-DMK: cellular distribution in human leukocyte populations and evidence of diurnal modulation.

J. Falgueyret, M. Percival, J. Gauthier, 2011, Analytical biochemistry.

Substituted coumarins as potent 5-lipoxygenase inhibitors.

J. Falgueyret, D. Riendeau, C. Brideau, 2006, Bioorganic & medicinal chemistry letters.

Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors.

J. Falgueyret, R. Oballa, J. Guay, 2011, Bioorganic & medicinal chemistry letters.

Sensitivity of immunoaffinity-purified porcine 5-lipoxygenase to inhibitors and activating lipid hydroperoxides.

J. Falgueyret, D. Riendeau, S. Yamamoto, 1989, Biochemical pharmacology.

Purification and characterization of recombinant microsomal prostaglandin E synthase-1.

J. Falgueyret, M. Percival, D. Riendeau, 2002, Protein expression and purification.

Synthesis of two analogues of arachidonic acid and their reactions with 12-Lipoxygenase

J. Falgueyret, D. Riendeau, J. Rokach, 1990 .

High-Throughput Scintillation Proximity Assay for Stearoyl-CoA Desaturase-1

J. Falgueyret, P. Tawa, Sébastien Guiral, 2011, Journal of biomolecular screening.

Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).

J. Falgueyret, R. Oballa, J. Guay, 2010, Bioorganic & medicinal chemistry letters.

2-Aryl benzimidazoles: human SCD1-specific stearoyl coenzyme-A desaturase inhibitors.

J. Falgueyret, R. Oballa, P. Tawa, 2010, Bioorganic & medicinal chemistry letters.

Design and synthesis of potent, isoxazole-containing renin inhibitors.

J. Falgueyret, M. Percival, Yongxin Han, 2012, Bioorganic & medicinal chemistry letters.

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.

J. Falgueyret, Yongxin Han, S. Gagné, 2011, Bioorganic & medicinal chemistry letters.

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.

J. Falgueyret, M. Percival, Yongxin Han, 2011, Bioorganic & medicinal chemistry letters.

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.

J. Falgueyret, M. Percival, Yongxin Han, 2011, Bioorganic & medicinal chemistry letters.

Stereoselective carbonyl reductases from rat skin and leukocyte microsomes converting 12‐ketoeicosatetraenoic acid to 12(S)‐HETE

J. Falgueyret, D. Riendeau, Y. Leblanc, 1990, FEBS letters.

Primary amides as selective inhibitors of cathepsin K.

C. Bayly, J. Falgueyret, M. Percival, 2007, Bioorganic & medicinal chemistry letters.

Quinolines as potent 5-lipoxygenase inhibitors: synthesis and biological profile of L-746,530.

J. Falgueyret, D. Riendeau, R. Young, 1998, Bioorganic & medicinal chemistry letters.

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.

J. Falgueyret, J. Palmer, M. Venuti, 2008, Bioorganic & medicinal chemistry letters.

Naphthalenic lignan lactones as selective, nonredox 5-lipoxygenase inhibitors. Synthesis and biological activity of (methoxyalkyl)thiazole and methoxytetrahydropyran hybrids.

J. Falgueyret, D. Riendeau, C. Brideau, 1994, Journal of medicinal chemistry.

Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic stability.

J. Falgueyret, D. Riendeau, C. Brideau, 1996, Journal of medicinal chemistry.

Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX‐2 inhibitor

J. Falgueyret, M. Percival, D. Riendeau, 1997, British journal of pharmacology.

Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2.

R Gordon, J. Falgueyret, M. Percival, 2001, The Journal of pharmacology and experimental therapeutics.

NAD(P)H-dependent reduction of 12-ketoeicosatetraenoic acid to 12(R)- and 12(S)-hydroxyeicosatetraenoic acid by rat liver microsomes.

J. Falgueyret, D. Riendeau, Y. Leblanc, 1988, Biochemical and biophysical research communications.

Inhibitor-induced changes in the intrinsic fluorescence of human cyclooxygenase-2.

J. Falgueyret, M. Percival, L. Passmore, 1996, Biochemistry.

N-(4-chlorophenyl)-N-hydroxy-N'-(3-chlorophenyl)urea, a general reducing agent for 5-, 12-, and 15-lipoxygenases and a substrate for their pseudoperoxidase activities.

J. Falgueyret, D. Riendeau, S. Desmarais, 1992, Biochemistry and cell biology = Biochimie et biologie cellulaire.

Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.

J. Falgueyret, R. Rydzewski, M. Percival, 2001, Journal of medicinal chemistry.

Identification of a potent and selective non-basic cathepsin K inhibitor.

J. Falgueyret, M. Mcgrath, M. Percival, 2006, Bioorganic & medicinal chemistry letters.

Characterization of the activity of purified recombinant human 5-lipoxygenase in the absence and presence of leukocyte factors.

J. Falgueyret, D. Riendeau, M. Abramovitz, 1991, The Journal of biological chemistry.

Evaluation of the role of conserved His and Met residues among lipoxygenases by site-directed mutagenesis of recombinant human 5-lipoxygenase.

J. Falgueyret, D. Riendeau, M. Abramovitz, 1991, The Journal of biological chemistry.

Assessing protein-RNA interactions using microfluidic capillary mobility shift assays.

J. Falgueyret, J. Fourtounis, C. Sayegh, 2011, Analytical biochemistry.

Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ.

J. Falgueyret, R. Stocco, Hugo Poirier, 2022, Journal of medicinal chemistry.

Quantitation of the lysosomotropic character of cationic amphiphilic drugs using the fluorescent basic amine Red DND-99.

J. Falgueyret, M. Percival, Jean-Pierre Falgueyret, 2004, Analytical biochemistry.

Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.

C. Bayly, J. Falgueyret, M. Percival, 2008, Journal of Medicinal Chemistry.

Development of a homogeneous immunoassay for the detection of angiotensin I in plasma using AlphaLISA acceptor beads technology.

J. Falgueyret, M. Percival, Steve Rowland, 2009, Analytical biochemistry.

Automethylation of protein arginine methyltransferase 6 (PRMT6) regulates its stability and its anti-HIV-1 activity

M. Wainberg, J. Falgueyret, P. Quashie, 2013, Retrovirology.

Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.

C. Bayly, J. Falgueyret, M. Percival, 2004, Bioorganic & medicinal chemistry letters.

Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.

J. Falgueyret, M. Percival, R. Young, 2005, Bioorganic & medicinal chemistry letters.

Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.

J. Falgueyret, M. Percival, R. Oballa, 2005, Journal of medicinal chemistry.

Altered sensitivity of aspirin-acetylated prostaglandin G/H synthase-2 to inhibition by nonsteroidal anti-inflammatory drugs.

J. Falgueyret, D. Riendeau, J. Mancini, 1997, Molecular pharmacology.

Zinc dependent activation of cAMP-specific phosphodiesterase (PDE4A).

J. Falgueyret, M. Percival, B. Yeh, 1997, Biochemical and biophysical research communications.

Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.

C. Bayly, J. Falgueyret, J. Palmer, 2006, Bioorganic & Medicinal Chemistry Letters.

Potency and selectivity of inhibition of cathepsin K, L and S by their respective propeptides.

J. Falgueyret, M. Percival, J. Mancini, 2000, European journal of biochemistry.

Oxidative bioactivation of the lactol prodrug of a lactone cyclooxygenase-2 inhibitor.

J. Falgueyret, D. Riendeau, Z. Wang, 1999, Drug metabolism and disposition: the biological fate of chemicals.

Overexpression of human prostaglandin G/H synthase-1 and -2 by recombinant vaccinia virus: inhibition by nonsteroidal anti-inflammatory drugs and biosynthesis of 15-hydroxyeicosatetraenoic acid.

J. Falgueyret, B. Kennedy, W. Cromlish, 1994, Molecular pharmacology.

Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816.

J. Falgueyret, D. Riendeau, C. Brideau, 1993, Journal of medicinal chemistry.

Mechanism of selective inhibition of human prostaglandin G/H synthase-1 and -2 in intact cells.

Jilly F. Evans, J. Falgueyret, D. Riendeau, 1996, Biochemical pharmacology.

Arginine 120 of Prostaglandin G/H Synthase-1 Is Required for the Inhibition by Nonsteroidal Anti-inflammatory Drugs Containing a Carboxylic Acid Moiety *

J. Falgueyret, D. Riendeau, J. Mancini, 1995, The Journal of Biological Chemistry.

Secretory protein 7B2 is associated with pancreatic hormones within normal islets and some experimentally induced tumors.

N. Seidah, M. Marcinkiewicz, S. Benjannet, 1988, Endocrinology.

Two-dimensional immunoblotting analysis and immunocytochemical localization of the secretory polypeptide 7B2 in adrenal medulla

M. Marcinkiewicz, S. Benjannet, J. Falgueyret, 1988, Neuroscience Letters.

The interaction of arginine 106 of human prostaglandin G/H synthase-2 with inhibitors is not a universal component of inhibition mediated by nonsteroidal anti-inflammatory drugs.

C. Bayly, J. Falgueyret, M. Percival, 1997, Molecular pharmacology.

Photo-crosslinking of proteins in intact cells reveals a dimeric structure of cyclooxygenase-2 and an inhibitor-sensitive oligomeric structure of microsomal prostaglandin E2 synthase-1.

Marc Ouellet, J. Falgueyret, D. Riendeau, 2008, Archives of biochemistry and biophysics.

Detergents profoundly affect inhibitor potencies against both cyclo-oxygenase isoforms.

J. Falgueyret, M. Percival, M. Ouellet, 2004, The Biochemical journal.

Automethylation of protein arginine methyltransferase 6 (PRMT6) regulates its stability and its anti-HIV-1 activity

M. Wainberg, J. Falgueyret, P. Quashie, 2013, Retrovirology.

Thiopyrano[2,3,4-cd]indoles as 5-lipoxygenase inhibitors: synthesis, biological profile, and resolution of 2-[2-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-4,5 -dihydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]ethoxy]butanoic acid.

J. Falgueyret, D. Riendeau, C. Brideau, 1994, Journal of Medicinal Chemistry.

Thiopyrano(2,3,4-cd)indoles as 5-Lipoxygenase Inhibitors: Synthesis, Biological Profile, and Resolution of 2-(2-(1-(4-Chlorobenzyl)-4- methyl-6-((5-phenylpyridin-2-yl)methoxy)-4,5-dihydro-1H-thiopyrano(2,3, 4-cd)indol-2-yl)ethoxy)butanoic Acid.

J. Falgueyret, D. Riendeau, C. Brideau, 1994 .

Photo-crosslinking of proteins in intact cells reveals a dimeric structure of cyclooxygenase-2 and an inhibitor-sensitive oligomeric structure of microsomal prostaglandin E2 synthase-1.

J. Falgueyret, D. Riendeau, M. Ouellet, 2008, Archives of biochemistry and biophysics.

Immunocytochemical localization of a novel pituitary polypeptide “7B2” in the gastro-intestinal tract of the rat

M. Marcinkiewicz, S. Benjannet, J. Falgueyret, 1987, Cell and Tissue Research.

The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.

J. Falgueyret, M. Percival, R. Oballa, 2010, Bioorganic & medicinal chemistry letters.