R. Marquis

发表

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.

Michelle C. Schaeffer, Carol A. Capriotti, P. A. Harris, 2017, Journal of medicinal chemistry.

A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys.

D. Veber, S. Kumar, D. Yamashita, 2007, Bone.

Inhibition of Invariant Chain Processing, Antigen-Induced Proliferative Responses, and the Development of Collagen-Induced Arthritis and Experimental Autoimmune Encephalomyelitis by a Small Molecule Cysteine Protease Inhibitor

John J. Peterson, D. Yamashita, R. Johanson, 2008, The Journal of Immunology.

Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.

Philip Hardwicke, John Bertin, Bryan W King, 2015, Bioorganic & medicinal chemistry.

Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.

Joseph P. Romano, N. C. Goodwin, J. Bertin, 2019, ACS medicinal chemistry letters.

Identification of Benzimidazole Diamides as Selective Inhibitors of the Nucleotide-Binding Oligomerization Domain 2 (NOD2) Signaling Pathway

J. Bertin, V. Kasparcova, Jong W. Yu, 2013, PloS one.

Identification of Selective Small Molecule Inhibitors of the Nucleotide-Binding Oligomerization Domain 1 (NOD1) Signaling Pathway

J. Bertin, V. Kasparcova, Zining Wu, 2014, PloS one.

MLKL compromises plasma membrane integrity by binding to phosphatidylinositol phosphates.

M. Bertrand, J. Bertin, P. Vandenabeele, 2014, Cell reports.

Potent and Selective Inhibition of Human Cathepsin K Leads to Inhibition of Bone Resorption In Vivo in a Nonhuman Primate

Y. Ru, D. Veber, K. Erhard, 2001, Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research.

Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.

R. DesJarlais, Y. Ru, M. Head, 1998, Journal of medicinal chemistry.

Antagonists of the calcium receptor. 2. Amino alcohol-based parathyroid hormone secretagogues.

B. Smith, K. Ward, Xiaoyang Dong, 2009, Journal of medicinal chemistry.

A potent small molecule, nonpeptide inhibitor of cathepsin K (SB 331750) prevents bone matrix resorption in the ovariectomized rat.

Y. Ru, D. Veber, K. Erhard, 2002, Bone.

Activation of PPARdelta alters lipid metabolism in db/db mice.

J. Auwerx, M. D. Leibowitz, D. Moller, 2000, FEBS letters.

Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues.

John C. Lee, B. Smith, K. Ward, 2009, Journal of medicinal chemistry.

High throughput screening identifies ATP-competitive inhibitors of the NLRP1 inflammasome.

P. A. Harris, J. Bertin, C. Duraiswami, 2015, Bioorganic & medicinal chemistry letters.

Toll-like Receptor 3-mediated Necrosis via TRIF, RIP3, and MLKL*

J. Bertin, C. Sehon, R. Marquis, 2013, The Journal of Biological Chemistry.

N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a Novel and Potent Transient Receptor Potential Vanilloid 4 Channel Agonist Induces Urinary Bladder Contraction and Hyperactivity: Part

D. Demarini, D. Brooks, N. Laping, 2008, Journal of Pharmacology and Experimental Therapeutics.

Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[ d]thiazol-5-ylamino)-6-( tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.

J. Bertin, K. Erhard, M. Convery, 2019, Journal of medicinal chemistry.

Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.

Michelle C. Schaeffer, Carol A. Capriotti, Paul E. Lamoureux, 2019, Journal of medicinal chemistry.

Synthesis of (S)-3-amino-benzo[b][1,4]oxazepin-4-one via Mitsunobu and SNAr reaction for a first-in-class RIP1 kinase inhibitor GSK2982772 in clinical trials

P. A. Harris, J. U. Jeong, Xiaoyang Dong, 2017 .

Design of amidobenzimidazole STING receptor agonists with systemic activity

Joseph P. Romano, J. Bertin, J. Adams, 2018, Nature.

GSK1016790A, a Novel and Potent TRPV4 Channel Agonist Induces Urinary Bladder Contraction and Hyperactivity: Part I

D. Demarini, D. Brooks, N. Laping, 2008 .

Cysteine Protease Inhibitor Encephalomyelitis by a Small Molecule Arthritis and Experimental Autoimmune the Development of Collagen-Induced andAntigen-Induced Proliferative Responses , Inhibition of Invariant Chain Processing

John J. Peterson, D. Yamashita, R. Johanson, 2008 .

Degradation of the C1 side chain of zaragozic acid A

R. Marquis, W. Parsons, G. D. Berger, 1994 .

Potent and Selective Cathepsin L Inhibitors Do Not Inhibit Human Osteoclast Resorption in Vitro *

Y. Ru, D. Veber, D. Yamashita, 2001, The Journal of Biological Chemistry.

Asymmetric synthesis of a potent azepanone-based inhibitor of the cysteine protease cathepsin K

R. Marquis, R. E. Trout, 2005 .

Procede d'inhibition de la cathepsine k

Baoguang Zhao, Y. Ru, D. Veber, 1996 .

Synthesis applications of cationic aza-Cope rearrangements. 24. The aza-Cope-Mannich approach to Strychnos alkaloids. Short stereocontrolled total syntheses of (.+-.)-dehydrotubifoline and (.+-.)-akuammicine

L. Overman, R. Marquis, S. R. Angle, 1993 .

Inhibition of the Cysteine Protease Cathepsin K (EC 3.4.22.38)

R. Marquis, 2004 .

Synthesis of tetrasubstituted pyrazines and pyrazine N-oxides

J. U. Jeong, Xiaoyang Dong, Attiq Rahman, 2010 .

Titanium(IV) isopropoxide mediated synthesis of pyrimidin-4-ones.

Yu-Bao Lan, R. Marquis, Michael P. Demartino, 2010, Organic letters.

Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.

Michelle C. Schaeffer, Carol A. Capriotti, P. A. Harris, 2013, ACS medicinal chemistry letters.

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.

Deepak Bandyopadhyay, Lauren Dare, Michelle C. Schaeffer, 2016, Journal of medicinal chemistry.

RIP3 induces apoptosis independent of pronecrotic kinase activity.

Kenta Moriwaki, Viera Kasparcova, John Bertin, 2014, Molecular cell.

Azepanone-based inhibitors of human and rat cathepsin K.

Y. Ru, D. Veber, K. Ward, 2001, Journal of medicinal chemistry.

Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.

Baoguang Zhao, M. Head, D. Veber, 2006, Journal of medicinal chemistry.

Cyclic ketone inhibitors of the cysteine protease cathepsin K.

Y. Ru, D. Veber, M. Hemling, 2001, Journal of medicinal chemistry.

Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.

J. Bertin, K. Erhard, D. Lipshutz, 2019 .

The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.

Carol A. Capriotti, J. Bertin, M. Convery, 2016, Journal of medicinal chemistry.

New approach to Strychnos alkaloids. Stereocontrolled total synthesis of (.+-.)-dehydrotubifoline

L. Overman, R. Marquis, J. Fevig, 1991 .

Synthesis Applications of Cationic Aza-Cope Rearrangements. Part 24. Aza-Cope-Mannich Approach to Strychnos Alkaloids. Short Stereocontrolled Total Syntheses of (.+-.)-Dehydrotubifoline and (.+-.) -Akuammicine.

L. Overman, R. Marquis, S. R. Angle, 1993 .

An Orally Active TRPV4 Channel Blocker Prevents and Resolves Pulmonary Edema Induced by Heart Failure

H. Alsaid, W. Bao, R. Willette, 2012, Science Translational Medicine.

Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.

J. Bertin, M. Convery, D. Lipshutz, 2018, ACS medicinal chemistry letters.

Design of amidobenzimidazole STING receptor agonists with systemic activity

J. Bertin, J. Adams, M. Bantscheff, 2018, Nature.

Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer

P. A. Harris, J. Bertin, M. Mahajan, 2019, ACS medicinal chemistry letters.

Author Correction: Design of amidobenzimidazole STING receptor agonists with systemic activity

Joseph P. Romano, J. Bertin, M. Bantscheff, 2019, Nature.

Activation of PPARδ alters lipid metabolism in db/db mice

J. Auwerx, M. D. Leibowitz, J. Berger, 2000 .

Chapter 28. Inhibition of cysteine proteases

R. Marquis, 2000 .

Systemic Activation of the Transient Receptor Potential Vanilloid Subtype 4 Channel Causes Endothelial Failure and Circulatory Collapse: Part 2

W. Bao, D. Behm, S. Nerurkar, 2008, Journal of Pharmacology and Experimental Therapeutics.

Novel Peroxisome Proliferator-activated Receptor (PPAR) γ and PPARδ Ligands Produce Distinct Biological Effects*

Margaret S. Wu, Y. Li, M. D. Leibowitz, 1999, The Journal of Biological Chemistry.

Overcoming the Pregnane X Receptor Liability: Rational Design to Eliminate PXR-Mediated CYP Induction.

Shawn P. Williams, Yu-Bao Lan, R. Marquis, 2021, ACS medicinal chemistry letters.

Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives.

R. Marquis, K. Bartizal, W. Parsons, 1994, Journal of medicinal chemistry.

An orally active calcium-sensing receptor antagonist that transiently increases plasma concentrations of PTH and stimulates bone formation.

B. Yi, S. Hoffman, R. Marquis, 2010, Bone.

Selective protection and relative importance of the carboxylic acid groups of zaragozic acid A for squalene synthase inhibition.

K. Wilson, R. Marquis, W. Parsons, 1994, Journal of medicinal chemistry.

Selective Protection and Relative Importance of the Carboxylic Acid Groups of Zargozic Acid A for Squalene Synthase Inhibition.

K. Wilson, R. Marquis, W. Parsons, 1994 .

Characterization of GSK′963: a structurally distinct, potent and selective inhibitor of RIP1 kinase

Michelle C. Schaeffer, Carol A. Capriotti, J. Bertin, 2015, Cell Death Discovery.

Understanding Pharmacokinetic Disconnect in Preclinical Species for 4-Aminoquinolines: Consequences of Low Permeability and High P-glycoprotein Efflux Ratio on Rat and Dog Oral Pharmacokinetics.

J. Bertin, M. Mahajan, R. Nagilla, 2020, Journal of pharmaceutical sciences.

MLKL compromises plasma membrane integrity by binding to phosphatidylinositol phosphates.

M. Bertrand, J. Bertin, P. Vandenabeele, 2014, Cell reports.

Azepanone-based inhibitors of human cathepsin L.

Y. Ru, M. Head, D. Veber, 2005, Journal of medicinal chemistry.

Diesters of zaragozic acid A: Synthesis and biological activity

R. Marquis, G. Doss, M. Kurtz, 1993 .

Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.

Carol A. Capriotti, J. Bertin, M. Convery, 2018, ACS medicinal chemistry letters.