J. Burke

发表

X‐Ray Crystal Structure of Bone Marrow Kinase in the X Chromosome: A Tec Family Kinase

D. Xie, J. Sack, Chiehying Y Chang, 2011, Chemical biology & drug design.

Collagen and Aggrecan Degradation Is Blocked in Interleukin-1-Treated Cartilage Explants by an Inhibitor of IκB Kinase through Suppression of Metalloproteinase Expression

J. Burke, M. Pattoli, J. Macmaster, 2005, Journal of Pharmacology and Experimental Therapeutics.

The cis-regulatory effect of an Alzheimer ' s disease-associated poly-T locus on expression of TOMM 40 and APOE genes

A. Roses, S. Saith, C. Linnertz, 2014 .

Inhibition of Protein Misfolding/Aggregation Using Polyglutamine Binding Peptide QBP1 as a Therapy for the Polyglutamine Diseases

W. Strittmatter, K. Wada, T. Takeuchi, 2013, Neurotherapeutics.

Expanded polyglutamine stretches form an ‘aggresome’

S. Tsuji, W. Strittmatter, T. Shimohata, 2002, Neuroscience 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.

Pharmacodynamics‐based approach for efficacious human dose projection of BMS‐986260, a small molecule transforming growth factor beta receptor 1 inhibitor

Y. Shu, R. Borzilleri, M. Cvijic, 2020, Biopharmaceutics & drug disposition.

IKK mediates ischemia-induced neuronal death

M. T. Hasan, H. Bujard, M. Köhrmann, 2005, Nature Medicine.

Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain

K. McIntyre, C. Chaudhry, L. Salter-Cid, 2019, Science Translational Medicine.

BMS-345541 Targets Inhibitor of κB Kinase and Induces Apoptosis in Melanoma: Involvement of Nuclear Factor κB and Mitochondria Pathways

J. Schmid, A. Richmond, Jinming Yang, 2006, Clinical Cancer Research.

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.

Pathogenesis of Inclusion Bodies in (CAG)n/Qn‐Expansion Diseases with Special Reference to the Role of Tissue Transglutaminase and to Selective Vulnerability

W. Strittmatter, J. Blass, G. Peluso, 1999, Journal of neurochemistry.

Leukotriene B4 stimulates the release of arachidonate in human neutrophils via the action of cytosolic phospholipase A2.

J. Burke, K. Tramposch, K. Gregor, 1997, Biochimica et biophysica acta.

Polyglutamine Domains Are Substrates of Tissue Transglutaminase: Does Transglutaminase Play a Role in Expanded CAG/Poly‐Q Neurodegenerative Diseases?

A. Roses, W. Strittmatter, J. Blass, 1997, Journal of neurochemistry.

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.

Duration and Intensity of NF-κB Activity Determine the Severity of Endotoxin-Induced Acute Lung Injury1

J. Christman, T. Blackwell, F. Yull, 2006, Journal of Immunology.

BMS-345541 targets inhibitor of kappaB kinase and induces apoptosis in melanoma: involvement of nuclear factor kappaB and mitochondria pathways.

J. Schmid, A. Richmond, Jinming Yang, 2006, Clinical cancer research : an official journal of the American Association for Cancer Research.

Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors.

K. McIntyre, M. Belema, Y. Qiu, 2007, Bioorganic & medicinal chemistry letters.

The multisubunit IkappaB kinase complex shows random sequential kinetics and is activated by the C-terminal domain of IkappaB alpha.

K. Miller, C. Meyers, J. Burke, 1998, The Journal of biological chemistry.

NEMO binding domain of IKK‐2 encompasses amino acids 735–745

C. Mapelli, D. Riexinger, R. Ryseck, 2006, Journal of molecular recognition : JMR.

Expanded Polyglutamine Domain Proteins Bind Neurofilament and Alter the Neurofilament Network

W. Strittmatter, O. Onodera, J. Chun, 1999, Experimental Neurology.

Oligomerization of expanded-polyglutamine domain fluorescent fusion proteins in cultured mammalian cells.

A. Roses, S. Tsuji, W. Strittmatter, 1997, Biochemical and biophysical research communications.

Polyglutamine Domain Proteins with Expanded Repeats Bind Neurofilament, Altering the Neurofilament Network

W. Strittmatter, O. Onodera, Y. Nagai, 1999, Annals of the New York Academy of Sciences.

Selectivity Profile of the Tyrosine Kinase 2 Inhibitor Deucravacitinib Compared with Janus Kinase 1/2/3 Inhibitors

Subhashish Banerjee, Qihong Zhao, M. Tagen, 2021, Dermatology and Therapy.

Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).

S. Spergel, K. McIntyre, J. Tokarski, 2019, Journal of medicinal chemistry.

349 - BMS-986165 is a Highly Potent and Selective Allosteric Inhibitor of TYK2, Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease

J. Chen, C. Chaudhry, K. Gillooly, 2018 .

Glyceraldehyde 3-Phosphate Dehydrogenase Abnormality in Metabolically Stressed Huntington Disease Fibroblasts

W. Strittmatter, J. Blass, Arthur J. L. Cooper, 1998, Developmental Neuroscience.

Interrelationships of Energy Metabolism to Oxidative Damage and Neurodegeneration

W. Strittmatter, J. Blass, Arthur James Cooper, 1998 .

Selective Inhibition of Tyrosine Kinase 2 With Deucravacitinib (BMS-986165) Compared With Janus Kinase 1−3 Inhibitors

Subhashish Banerjee, J. Throup, J. Burke, 2020 .

Targeting I kappa B kinase for the treatment of inflammatory and other disorders.

J. Burke, 2003, Current opinion in drug discovery & development.

Competitive, Reversible Inhibition of Cytosolic Phospholipase A2 at the Lipid-Water Interface by Choline Derivatives That Partially Partition into the Phospholipid Bilayer*

M. Witmer, J. Villafranca, R. Padmanabha, 1999, The Journal of Biological Chemistry.

Differentiation of U937 cells enables a phospholipase D-dependent pathway of cytosolic phospholipase A2 activation.

J. Burke, K. Gregor, L. Davern, 1999, Biochemical and biophysical research communications.

The size and curvature of anionic covesicle substrate affects the catalytic action of cytosolic phospholipase A2.

M. Witmer, J. Burke, J. Tredup, 1999, Archives of biochemistry and biophysics.

A beta-lactam inhibitor of cytosolic phospholipase A2 which acts in a competitive, reversible manner at the lipid/water interface.

M. Witmer, R. Padmanabha, S. Manly, 1998, Journal of enzyme inhibition.

Phosphorylation and calcium influx are not sufficient for the activation of cytosolic phospholipase A2 in U937 cells: requirement for a Gi alpha-type G-protein.

G. Todderud, J. Burke, K. Tramposch, 1997, Biochimica et biophysica acta.

Presence of glycerol masks the effects of phosphorylation on the catalytic efficiency of cytosolic phospholipase A2.

M. Witmer, M. Guenther, J. Villafranca, 1997, Archives of biochemistry and biophysics.

Dicarboxylic acid inhibitors of phospholipase A2

P. Stanley, J. Burke, J. Bronson, 1997 .

Acute Lung Injury Endotoxin-InducedDetermine the Severity of B Activity κ Duration and Intensity of NF -

J. Christman, T. Blackwell, F. Yull, 2006 .

A High-Throughput BRET Cellular Target Engagement Assay Links Biochemical to Cellular Activity for Bruton’s Tyrosine Kinase

B. Arey, C. Chaudhry, A. Tebben, 2019, SLAS discovery : advancing life sciences R & D.

Periodic, Partial Inhibition of IκB Kinase β-Mediated Signaling Yields Therapeutic Benefit in Preclinical Models of Rheumatoid Arthritis

K. McIntyre, Laishun Chen, W. Pitts, 2009, Journal of Pharmacology and Experimental Therapeutics.

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.

S. Spergel, R. Moquin, K. McIntyre, 2009, Bioorganic & medicinal chemistry letters.

Phage display screening for peptides that inhibit polyglutamine aggregation.

W. Strittmatter, D. Kenan, J. Burke, 2006, Methods in enzymology.

An inhibitor of IκB kinase, BMS-345541, blocks endothelial cell adhesion molecule expression and reduces the severity of dextran sulfate sodium-induced colitis in mice

D. Dambach, Y. Qiu, D. Lee, 2003, Inflammation Research.

BMS-229724 is a tight-binding inhibitor of cytosolic phospholipase A2 that acts at the lipid/water interface and possesses anti-inflammatory activity in skin inflammation models.

P. Stanley, M. Witmer, P. Brassil, 2001, The Journal of pharmacology and experimental therapeutics.

Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).

K. McIntyre, J. Barrish, A. Mathur, 2016, Journal of medicinal chemistry.

Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).

David S. Nirschl, David S Nirschl, Michael A. Galella, 2011, Bioorganic & medicinal chemistry letters.

Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.

David S. Nirschl, David S Nirschl, S. Spergel, 2011, Bioorganic & medicinal chemistry letters.

An inhibitor of IkappaB kinase, BMS-345541, blocks endothelial cell adhesion molecule expression and reduces the severity of dextran sulfate sodium-induced colitis in mice.

D. Dambach, D. Lee, J. Burke, 2003, Inflammation research : official journal of the European Histamine Research Society ... [et al.].

Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.

Michael A. Galella, K. McIntyre, J. Barrish, 2020, ACS medicinal chemistry letters.

Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.

J. Tokarski, D. Xie, N. Araníbar, 2017, MedChemComm.

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.

Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.

James Lin, K. McIntyre, J. Tokarski, 2019, ACS medicinal chemistry letters.

BMS-345541 Is a Highly Selective Inhibitor of IκB Kinase That Binds at an Allosteric Site of the Enzyme and Blocks NF-κB-dependent Transcription in Mice*

James R. Burke, John F. MacMaster, K. McIntyre, 2003, The Journal of Biological Chemistry.

Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain*

Stephen R. Johnson, M. Witmer, J. Tokarski, 2015, The Journal of Biological Chemistry.

Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked

Michael A. Galella, K. McIntyre, J. Barrish, 2016, Journal of medicinal chemistry.

Cooperativity and binding in the mechanism of cytosolic phospholipase A2.

M. Witmer, J. Lahiri, J. Villafranca, 1995, Biochemistry.

IKK-2/NF-κB-DEPENDENT TRANSCRIPTION

W. Pitts, J. Burke, F. C. Zusi, 2007 .

Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries.

E. Toone, W. Strittmatter, D. Sane, 2008, Chemistry & biology.

Early mitochondrial calcium defects in Huntington's disease are a direct effect of polyglutamines

James R. Burke, Blair R. Leavitt, Claire-Anne Gutekunst, 2002, Nature Neuroscience.

Inhibition of Polyglutamine Protein Aggregation and Cell Death by Novel Peptides Identified by Phage Display Screening*

James R. Burke, Yoshitaka Nagai, Jack D. Keene, 2000, The Journal of Biological Chemistry.

Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).

Michael A. Galella, K. McIntyre, J. Macor, 2019, Journal of medicinal chemistry.

Bruton's tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care

K. McIntyre, A. Fura, K. Gillooly, 2017, PloS one.

Chronic cisplatin treatment promotes enhanced damage repair and tumor progression in a mouse model of lung cancer.

Katherine S. Lovejoy, T. Golub, A. Subramanian, 2010, Genes & development.

tumor progression in a mouse model of lung cancer Chronic cisplatin treatment promotes enhanced damage repair and Material

Katherine S. Lovejoy, T. Golub, A. Subramanian, 2010 .

Generation of Neuronal Intranuclear Inclusions by Polyglutamine-GFP: Analysis of Inclusion Clearance and Toxicity as a Function of Polyglutamine Length

K. Moulder, W. Strittmatter, O. Onodera, 1999, The Journal of Neuroscience.

Caspase-2-mediated cleavage of Mdm2 creates a p53-induced positive feedback loop.

T. Jacks, W. Xue, D. Hubbard, 2011, Molecular cell.

BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice.

K. McIntyre, Y. Qiu, F Christopher Zusi, 2003, The Journal of biological chemistry.

IκB kinase inhibitors for treating autoimmune and inflammatory disorders: potential and challenges

J. Strnad, J. Burke, 2007 .

Toxicity of expanded polyglutamine‐domain proteins in Escherichia coli

J. Vance, S. Tsuji, W. Strittmatter, 1996, FEBS letters.

The Aggregation Inhibitor Peptide QBP1 as a Therapeutic Molecule for the Polyglutamine Neurodegenerative Diseases

W. Strittmatter, K. Wada, T. Takeuchi, 2011, Journal of amino acids.

Prevention of polyglutamine oligomerization and neurodegeneration by the peptide inhibitor QBP1 in Drosophila.

W. Strittmatter, M. Yamaguchi, T. Toda, 2003, Human molecular genetics.

The Haw River Syndrome: Dentatorubropallidoluysian atrophy (DRPLA) in an African–American family

M. Pericak-Vance, A. Roses, J. Vance, 1994, Nature Genetics.

Synthesis and structure–activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-β inhibitors

K. McIntyre, K. Gillooly, M. Belema, 2007 .

Peptides Corresponding to the N and C Termini of IκB-α, -β, and -ε as Probes of the Two Catalytic Subunits of IκB Kinase, IKK-1 and IKK-2*

R. Ryseck, S. Walther, C. Meyers, 1999, The Journal of Biological Chemistry.

Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.

C. Chaudhry, P. Carter, Neha Surti, 2018, Bioorganic & medicinal chemistry letters.

Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).

Zheng Yang, Neha Surti, Jonathan S Lippy, 2015, Bioorganic & medicinal chemistry letters.

Amino acid sequence requirements of peptides that inhibit polyglutamine-protein aggregation and cell death.

W. Strittmatter, Y. Nagai, J. Burke, 2001, Biochemical and biophysical research communications.

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

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

Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy- N-

David S Nirschl, Michael A. Galella, S. Spergel, 2012 .

Novel tricyclic inhibitors of IkappaB kinase.

David S Nirschl, S. Spergel, R. Moquin, 2009, Journal of medicinal chemistry.

Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.

Andrew Tebben, Qian Ruan, Neha Surti, 2014, Bioorganic & medicinal chemistry letters.

Determination of Real Time in Vivo Drug Receptor Occupancy for a Covalent Binding Drug as a Clinical Pharmacodynamic Biomarker by Immunocapture-LC-MS/MS.

Robert J. Neely, Yan J. Zhang, B. Warrack, 2019, Analytical chemistry.

Targeting phospholipase A2 for the treatment of inflammatory skin diseases.

J. Burke, 2001, Current opinion in investigational drugs.

IkappaB kinase inhibitors for treating autoimmune and inflammatory disorders: potential and challenges.

J. Strnad, J. Burke, 2007, Trends in pharmacological sciences.

Inhibition of α-ketoglutarate-and pyruvate dehydrogenase complexes in E. coli by a glutathione S-transferase containing a pathological length poly-Q domain: A possible role of energy deficit in neurological diseases associated with poly-Q expansions?

James R. Burke, John P. Blass, Osamu Onodera, 1998, AGE.

Disruption of the toxic conformation of the expanded polyglutamine stretch leads to suppression of aggregate formation and cytotoxicity.

W. Strittmatter, Y. Urade, T. Toda, 2004, Biochemical and biophysical research communications.

In vitro effects of polyglutamine tracts on Ca2+-dependent depolarization of rat and human mitochondria: relevance to Huntington's disease.

W. Strittmatter, A. Panov, J. Burke, 2003, Archives of biochemistry and biophysics.

Disrupted Spermine Homeostasis: A Novel Mechanism in Polyglutamine-Mediated Aggregation and Cell Death

J. Wakefield, W. Strittmatter, C. Colton, 2004, The Journal of Neuroscience.

The Multisubunit IκB Kinase Complex Shows Random Sequential Kinetics and Is Activated by the C-terminal Domain of IκBα*

K. Miller, C. Meyers, J. Burke, 1998, The Journal of Biological Chemistry.

Transglutaminase-catalyzed inactivation of glyceraldehyde 3-phosphate dehydrogenase and alpha-ketoglutarate dehydrogenase complex by polyglutamine domains of pathological length.

A. Roses, W. Strittmatter, J. Blass, 1997, Proceedings of the National Academy of Sciences of the United States of America.

Polyglutamine expansion inhibits respiration by increasing reactive oxygen species in isolated mitochondria.

W. Strittmatter, K. Puranam, J. Burke, 2006, Biochemical and biophysical research communications.

Inhibition of Protein Misfolding/Aggregation Using Polyglutamine Binding Peptide QBP1 as a Therapy for the Polyglutamine Diseases

W. Strittmatter, K. Wada, T. Takeuchi, 2013, Neurotherapeutics.

Optimization of a polyglutamine aggregation inhibitor peptide (QBP1) using a thioflavin T fluorescence assay.

W. Strittmatter, Guangtao Zhang, J. Burke, 2007, Assay and drug development technologies.

Cytosolic phospholipase A2 shows burst kinetics consistent with the slow, reversible formation of a dead-end complex.

M. Witmer, M. Guenther, J. Burke, 2002, Archives of biochemistry and biophysics.

Peptides corresponding to the N and C termini of IkappaB-alpha, -beta, and -epsilon as probes of the two catalytic subunits of IkappaB kinase, IKK-1 and IKK-2.

R. Ryseck, S. Walther, C. Meyers, 1999, The Journal of biological chemistry.

Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.

K. McIntyre, K. Gillooly, M. Belema, 2007, Bioorganic & Medicinal Chemistry Letters.

Mechanism of Inhibition of Human Nonpancreatic Secreted Phospholipase A by the Anti-inflammatory Agent BMS-181162 (*)

J. Burke, K. Tramposch, K. Gregor, 1995, The Journal of Biological Chemistry.

Duration and Intensity of NF-κB Activity Determine the Severity of Endotoxin-Induced Acute Lung Injury1

J. Christman, T. Blackwell, F. Yull, 2006, The Journal of Immunology.

Reply to “A role for GAPDH in apoptosis and neurodegeneration”

A. Roses, J. Vance, W. Strittmatter, 1996, Nature Medicine.

Traitement de maladies neurodegeneratives

W. Strittmatter, C. Colton, M. Vitek, 2006 .