D. Shuster

发表

Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

Ping Chen, A. Doweyko, Derek J. Norris, 2004, Journal of medicinal chemistry.

2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase in

Ping Chen, A. Doweyko, Derek J. Norris, 2006, Journal of medicinal chemistry.

5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.

Gulzar Ahmed, Arthur M Doweyko, Axel Metzger, 2005, Journal of medicinal chemistry.

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.

James Lin, K. McIntyre, D. Shuster, 2015, Journal of medicinal chemistry.

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.

A. Doweyko, K. McIntyre, D. Shuster, 2011, Bioorganic & medicinal chemistry letters.

A HIGHLY SELECTIVE INHIBITOR OF IκB KINASE, BMS-345541, AUGMENTS GRAFT SURVIVAL MEDIATED BY SUBOPTIMAL IMMUNOSUPPRESSION IN A MURINE MODEL OF CARDIAC GRAFT REJECTION

K. McIntyre, D. Shuster, Y. Qiu, 2004, Transplantation.

Absence of OATP1B Induction by Rifampin in Cynomolgus Monkeys: Determination Using the Endogenous OATP1B Marker Coproporphyrin and Tissue Gene Expression

D. Shuster, Yueping Zhang, M. Sinz, 2020 .

Absence of OATP1B (Organic Anion–Transporting Polypeptide) Induction by Rifampin in Cynomolgus Monkeys: Determination Using the Endogenous OATP1B Marker Coproporphyrin and Tissue Gene Expression

D. Shuster, Shenjue Chen, Yueping Zhang, 2020, The Journal of Pharmacology and Experimental Therapeutics.

Transcriptional Profiling of Liver and Effect of Glucocorticoids in a Rat Adjuvant-Induced Arthritis Model

D. Shuster, V. Sasseville, S. Nadler, 2011, Veterinary pathology.

Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.

D. Shuster, J. Macor, J. Yanchunas, 2020, Journal of medicinal chemistry.

A highly selective inhibitor of I kappa B kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice.

K. McIntyre, D. Shuster, D. Dambach, 2003, Arthritis and rheumatism.

IL-1 receptor accessory protein is an essential component of the IL-1 receptor.

K. McIntyre, D. Shuster, M. Labow, 1998, Journal of immunology.

This information is current as Essential Component of the IL-1 Receptor IL-1 Receptor Accessory Protein Is an

K. McIntyre, D. Shuster, M. Labow, 1998 .

Insertion of a Structural Domain of Interleukin (IL)-1β Confers Agonist Activity to the IL-1 Receptor Antagonist

K. McIntyre, D. Shuster, S. Greenfeder, 1995, The Journal of Biological Chemistry.

Selective Itk inhibitors block T-cell activation and murine lung inflammation.

A. Doweyko, S. Spergel, R. Moquin, 2004, Biochemistry.

Tricyclic Sulfones as Potent, Selective and Efficacious RORγt Inverse Agonists - Exploring C6 and C8 SAR Using Late-Stage Functionalization.

Michael G. Yang, D. Shuster, C. Weigelt, 2020, Bioorganic & medicinal chemistry letters.

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

A. Doweyko, James Lin, J. Wityak, 2010, Journal of medicinal chemistry.

Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.

A. Doweyko, S. Spergel, R. Moquin, 2006, Bioorganic & medicinal chemistry letters.

Improving the pharmacokinetic and CYP inhibition profiles of azaxanthene-based glucocorticoid receptor modulators-identification of (S)-5-(2-(9-fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)-5H-chromeno[2,3-b]pyridin-5-yl)-2-methylpropanamido)-N-(tetrahydro-2H-pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide

Michael G. Yang, Michael A. Galella, K. McIntyre, 2015, Journal of medicinal chemistry.

Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-7918

A. Doweyko, D. Shuster, J. Barrish, 2011, Journal of medicinal chemistry.

C-3 Amido-indole cannabinoid receptor modulators.

Ping Chen, Derek J. Norris, K. McIntyre, 2002, Bioorganic & medicinal chemistry letters.

Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419).

Ping Chen, Henry H. Gu, E. Iwanowicz, 2007, Journal of medicinal chemistry.

Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.

Michael G. Yang, A. Doweyko, D. Shuster, 2014, Bioorganic & medicinal chemistry letters.

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.

Michael A. Galella, D. Shuster, D. Shen, 2019, ACS medicinal chemistry letters.

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.

S. Spergel, K. McIntyre, D. Shuster, 2019, Journal of medicinal chemistry.

Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.

Ping Chen, Derek J. Norris, S. Spergel, 2003, Journal of medicinal chemistry.

Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.

A. Doweyko, K. McIntyre, D. Shuster, 2008, Bioorganic & medicinal chemistry letters.

Dimethyl-diphenyl-propanamide derivatives as nonsteroidal dissociated glucocorticoid receptor agonists.

A. Doweyko, D. Shuster, J. Barrish, 2010, Journal of medicinal chemistry.

Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.

John Dodd, John S Tokarski, Arthur M Doweyko, 2008, Journal of medicinal chemistry.

An LFA-1 (αLβ2) Small-Molecule Antagonist Reduces Inflammation and Joint Destruction in Murine Models of Arthritis

P. M. Davis, K. McIntyre, D. Shuster, 2010, The Journal of Immunology.

Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.

Michael G. Yang, D. Shuster, C. Weigelt, 2021, ACS medicinal chemistry letters.

Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.

D. Shuster, J. Macor, C. Weigelt, 2020, ACS medicinal chemistry letters.

Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

Ping Chen, A. Doweyko, Derek J. Norris, 2004, Bioorganic & medicinal chemistry letters.

Absence of IL-1 signaling and reduced inflammatory response in IL-1 type I receptor-deficient mice.

K. McIntyre, D. Shuster, M. Labow, 1997, Journal of immunology.

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Wei Li, Gulzar Ahmed, John Dodd, 2004, Journal of medicinal chemistry.

Liquid chromatography coupled with tandem mass spectrometry for the bioanalysis of proteins in drug development: practical considerations in assay development and validation.

Qin C Ji, Guowen Liu, Mark Arnold, 2013, Journal of chromatography. A.

Reduced incidence and severity of collagen‐induced arthritis in interleukin‐12‐deficient mice

K. McIntyre, D. Shuster, M. Gately, 1996, European journal of immunology.

Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.

James Lin, K. McIntyre, D. Shuster, 2020, Journal of medicinal chemistry.

Characterization of E-selectin-deficient mice: demonstration of overlapping function of the endothelial selectins.

K. McIntyre, D. Shuster, M. Labow, 1994, Immunity.

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

A. Doweyko, S. Spergel, R. Moquin, 2006, Bioorganic & medicinal chemistry letters.

Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design.

K. McIntyre, D. Shuster, D. Shen, 2016, Journal of medicinal chemistry.

Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.

S. Spergel, R. Moquin, K. McIntyre, 2016, Journal of medicinal chemistry.

Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).

S. Spergel, K. McIntyre, D. Shuster, 2016, Bioorganic & medicinal chemistry letters.

Assessment of tissue biomarkers following anti-CD137 treatment in the EMT-6 mouse tumor model.

D. Shuster, Z. Tsuchihashi, M. Jure-Kunkel, 2006 .

Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt ‒ Identification of a Potent, Selective Series with Biologic-Like In Vivo Efficacy.

K. McIntyre, D. Shuster, J. Macor, 2019, Journal of medicinal chemistry.

Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.

D. Shuster, J. Macor, C. Weigelt, 2020, ACS medicinal chemistry letters.

Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity.

D. Cheney, Henry H. Gu, E. Iwanowicz, 2002, Journal of medicinal chemistry.

Dual Inhibition of Interleukin-23 and Interleukin-17 Offers Superior Efficacy in Mouse Models of Autoimmunity

Noah T. Ditto, M. Struthers, K. McIntyre, 2015, The Journal of Pharmacology and Experimental Therapeutics.

Creation and characterization of E-selectin- and VCAM-1-deficient mice.

D. Shuster, C. Stewart, C. Norton, 1995, Ciba Foundation symposium.

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.

A. Doweyko, K. McIntyre, D. Shuster, 2008, Bioorganic & medicinal chemistry letters.

Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.

Michael G. Yang, D. Shuster, C. Weigelt, 2021, Journal of medicinal chemistry.

Quantification of human mAbs in mouse tissues using generic affinity enrichment procedures and LC-MS detection.

D. Shuster, S. Rajendran, T. Olah, 2014, Bioanalysis.