publications

IMMUNOLOGY

• Effects of Fostamatinib (R788), an Oral Spleen Tyrosine Kinase Inhibitor, on Health-related Quality of Life in Patients with Active Rheumatoid Arthritis: Analyses of Patient-reported Outcomes from a Randomized, Double-blind, Placebo-controlled Trial
  
  
• Significant Reduction of Acute Cardiac Allograft Rejection by Selective Janus Kinase-1/3 Inhibition Using R507 and R545
  
  
• Spleen Tyrosine Kinase Is Important in the Production of Proinflammatory Cytokines and Cell Proliferation in Human Mesangial Cells following Stimulation with IgA1 Isolated from IgA Nephropathy Patients
  
  
• Inhibition of Syk activity by R788 in platelets prevents remote lung tissue damage after mesenteric ischemia-reperfusion injury
  
  
• Fostamatinib, a syk-kinase inhibitor, does not affect methotrexate pharmacokinetics in patients with rheumatoid arthritis
  
  
• The oral spleen tyrosine kinase inhibitor fostamatinib attenuates inflammation and atherogenesis in low-density lipoprotein receptor-deficient mice
  
  
• An oral spleen tyrosine kinase (Syk) inhibitor for rheumatoid arthritis - TASKi2
  
  
• An oral Syk kinase inhibitor in the treatment of rheumatoid arthritis - TASKi3
  
  
• Spleen tyrosine kinase inhibition prevents tissue damage after ischemia-reperfusion
  
  
• Therapeutic Targeting of Syk in Autoimmune Diabetes
  
  
• Suppression of skin and kidney disease by inhibition of spleen tyrosine kinase in lupus-prone mice
  
  
• Metabolism of fostamatinib, the oral methylene phosphate prodrug of the spleen tyrosine kinase inhibitor R406 in humans
  
  
• Contribution of gut bacteria to the metabolism of the spleen tyrosine kinase (Syk) inhibitor R406 in cynomolgus monkey
  
  
• A Spleen Tyrosine Kinase Inhibitor Reduces the Severity of Established Glomerulonephritis
  
  
• A novel JAK3 inhibitor, R348, attenuates chronic airway allograft rejection
  
  
• JAK3 inhibition significantly attenuates Psoriasiform skin inflammation in CD18 mutant PL/J mice
  
  
• Of mice and men: an open label pilot study for treatment of immune thrombocytopenic purpura (ITP) by an inhibitor of Syk.
  
  
• Differential expression and molecular associations of Syk in systemic lupus erythermatosus T cells.
  
  
• Treatment of rheumatoid arthritis with a syk kinase inhibitor: A twelve-week, randomized, placebo-controlled trial.
  
  
• An orally bioavailable spleen tyrosine kinase inhibitor delays disease progression and prolongs survival in murine lupus.
  
  
• A Class of Small Molecules that Inhibit TNFalpha-Induced Survival and Death Pathways via Prevention of Interactions between TNFalphaRI, TRADD, and RIP1.
  
  
• Inflammation and bone erosion are suppressed in models of rheumatoid arthritis following treatment with a novel Syk inhibitor.
  
  
• Syk inhibitors as treatment for allergic rhinitis.
  
  
• R406, an orally available spleen tyrosine kinase inhibitor, blocks fc receptor signaling and reduces immune complex-mediated inflammation.
  
  
• Identification of the Syk kinase inhibitor R112 by a human mast cell screen.
  
  
• Inhibition of spleen tyrosine kinase prevents mast cell activation and airway hyperresponsiveness.
  
  
• An intranasal Syk-kinase inhibitor improves the symptoms of seasonal allergic rhinitis in a park environment.
  
  
• Targeting Syk as a treatment for allergic and autoimmune disorders.
  
  
• A novel role for p21-activated protein kinase 2 in T cell activation.
  
  
• A novel E3 ubiquitin ligase TRAC-1 positively regulates T cell activation.
  
  
• Systematic identification of regulatory proteins critical for T cell activation.
  
  
• Retrovirally delivered random cyclic peptide libraries yield inhibitors of interleukin-4 signaling in human B cells.
  
  
• Functional cloning of Src-like adapter protein-2 (SLAP-2), a novel inhibitor of antigen receptor signaling.
  
  
• Cytokine regulation of liver development.
  
  
• Toso, a cell surface-specific regulator of Fas-induced apoptosis in T cells.
  
  
• SWAP-70-deficient mast cells are impaired in development and IgE-mediated degranulation.
  
  
• Rab37 is a novel mast cell specific GTPase localized to secretory granules.
  
  
• Association of SWAP-70 with the B cell antigen receptor complex.
  
  
• Quantitative measurement of mast cell degranulation using a novel flow cytometric annexin-V binding assay.
  
  
• Amisyn, a novel syntaxin-binding protein that may regulate SNARE complex assembly.
  
  
• "Syniping" away at glucose transport.
  
  
• Three novel proteins of the syntaxin/SNAP-25 family.
  
  
• Tomosyn binds t-SNARE proteins via a VAMP-like coiled coil.

ONCOLOGY

• R723, a selective JAK2 inhibitor, effectively treats JAK2V617F-induced murine myeloproliferative neoplasm
  
  
• The Axl receptor tyrosine kinase is an adverse prognostic factor and a therapeutic target in esophageal adenocarcinoma
  
  
• Inhibition of Syk with fostamatinib disodium has significant clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia
  
  
• The current status and the future of JAK2 inhibitors for the treatment of myeloproliferative diseases
  
  
• R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer
  
  
• Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen
  
  
• Mouse models of non-Hodgkins lymphoma reveal Syk as an important therapeutic target.
  
  
• Ribosomal protein S6 is a selective mediator of TRAIL-apoptotic signaling.
  
  
• R-253 disrupts microtubule networks in multiple tumor cell lines.
  
  
• Multiple roles for the receptor tyrosine kinase axl in tumor formation.
  
  
• Critical role of the ubiquitin ligase activity of UHRF1, a nuclear RING finger protein, in tumor cell growth.
  
  
• Cell cycle regulatory E3 ubiquitin ligases as anticancer targets.
  
  
• The poxvirus p28 virulence factor is an E3 ubiquitin ligase.
  
  
• Identification and functional characterization of a novel human misshapen/Nck interacting kinase-related kinase, hMINK beta.
  
  
• Cellular localization and anti-proliferative effect of peptides discovered from a functional screen of a retrovirally-delivered random peptide library.
  
  
• Utility of peptide-protein affinity complexes in proteomics: identification of interaction partners of a tumor suppressor peptide.
  
  
• MAPKK-independent activation of p38alpha mediated by TAB1-dependent autophosphorylation of p38alpha.
  
  
• Activation of the PKB/AKT pathway by ICAM-2.
  
  
• p15(PAF), a novel PCNA associated factor with increased expression in tumor tissues.
  
  
• Identification of RIP3, a RIP-like kinase that activates apoptosis and NFkB.
  
  
• Detection of programmed cell death using fluorescence energy transfer.

VIROLOGY

• Discovery and Characterization of Substituted Diphenyl Heterocyclic Compounds as Potent and Selective Inhibitors of Hepatitis C Virus Replication.
  
  
• Riboproteomics of the hepatitis C virus internal ribosomal entry site.
  
  

LIGASES

• Approaches to discovering drugs that regulate E3 ubiquitin ligases
  
  
• Substrate modification with lysine 63-linked ubiquitin chains through the UBC13-UEV1A ubiquitin-conjugating enzyme
  
  
• Evaluation of a diffusion-driven mechanism for substrate ubiquitination by the SCF-Cdc34 ubiquitin ligase complex.
  
  
• Mechanism of lysine 48-linked ubiquitin-chain synthesis by the cullin-RING ubiquitin-ligase complex SCF-Cdc34.
  
  
• Critical role of the ubiquitin ligase activity of UHRF1, a nuclear RING finger protein, in tumor cell growth.
  
  
• High-Throughput Screening for Inhibitors of the E3 Ubiquitin Ligase APC.
  
  
• A Homogeneous FRET Assay System for Multiubiquitin Chain Assembly and Disassembly.
  
  
• A novel E3 ubiquitin ligase TRAC-1 positively regulates T cell activation.
  
  
• The poxvirus p28 virulence factor is an E3 ubiquitin ligase.
  
  
• Multiple functional categories of proteins identified in an in vitro cellular ubiquitin affinity extract using shotgun peptide sequencing.
  
  
• Drug discovery in the ubiquitin regulatory pathway.
  
  
• Cell cycle regulatory E3 ubiquitin ligases as anticancer targets.

Chemistry

• Diverse alkaloid-like structures from a common building block.
  
  
• General Route for the Preparation of Diverse 17-Membered Macrocycles Based on RCM and Examination of the E/Z Selectivity
  
  
• Discovery and Development of Spleen Tyrosine Kinase (SYK) Inhibitors
  
  

Flow Cytometry

• Characterization and use of green fluorescent proteins from Renilla mulleri and Ptilosarcus guernyi for the human cell display of functional peptides.
  
  
• Quantitative measurement of mast cell degranulation using a novel flow cytometric annexin-V binding assay.
  
  
• Detection of programmed cell death using fluorescence energy transfer.

Informatics

• Discovering patterns to extract protein-protein interactions from full texts.
  
  
• Computational and experimental studies on human misshapen/NIK-related kinase MINK-1.

Peptide Screens

• Gas phase dimerization of neuropeptide head activator analogs useful for the noncovalent constraint of peptides.
  
  
• Stable, stoichiometric delivery of diverse protein functions.
  
  
• Dominant effector genetics in mammalian cells.
  
  
• Cellular localization and anti-proliferative effect of peptides discovered from a functional screen of a retrovirally-delivered random peptide library.
  
  
• Utility of peptide-protein affinity complexes in proteomics: identification of interaction partners of a tumor suppressor peptide.
  
  
• Retrovirally delivered random cyclic peptide libraries yield inhibitors of interleukin-4 signaling in human B cells.
  
  
• Characterization and use of green fluorescent proteins from Renilla mulleri and Ptilosarcus guernyi for the human cell display of functional peptides.
  
  
• Intracellular protein scaffold-mediated display of random peptide libraries for phenotypic screens in mammalian cells.
  
  
• A novel artificial loop scaffold for the noncovalent constraint of peptides.
  
  
• Retroviral delivery of peptide modulators of cellular functions.
  
  
• Intracellular combinatorial chemistry with peptides in selection of caspase-like inhibitors.

Proteomics

• Riboproteomics of the hepatitis C virus internal ribosomal entry site.
  
  
• A new algorithm for the evaluation of shotgun peptide sequencing in proteomics: support vector machine classification of peptide MS/MS spectra and SEQUEST scores.
  
  
• Use of MEDUSA-based data analysis and capillary HPLC-ion-trap mass spectrometry to examine complex immunoaffinity extracts of RBAp48.
  
  
• Multidimensional data integration and relationship inference.

Retroviral Approaches

• A retroviral-mediated approach to functional screening: isolation of genetic effectors using a tetracycline-conditional system.
  
  
• Optimization of regulated LTR-mediated expression.
  
  
• The use of retroviruses as pharmaceutical tools for target discovery and validation in the field of functional genomics.
  
  
• Rapid production of retroviruses for efficient gene delivery to mammalian cells using 293T cell-based systems.

Signal Transduction

• Discovery and development of an aurora kinase inhibitor clinical candidate using an image-based assay for measuring proliferation, apoptosis, and DNA content.
  
  
• Cambridge Healthtech Institute Signal Transduction Conference: targets for effective therapeutics.
  
  
• TNIK, a novel member of the germinal center kinase family that activates the c-Jun N-terminal kinase pathway and regulates the cytoskeleton.

Yeast Two-Hybrid

• Yeast one and two hybrid cDNA cloning.