T. Angeles

发表

The chemopreventive agent oltipraz possesses potent antiangiogenic activity in vitro, ex vivo, and in vivo and inhibits tumor xenograft growth.

B. Ruggeri, M. Clapper, C. Robinson, 2002, Clinical cancer research : an official journal of the American Association for Cancer Research.

Comparison of LanthaScreen Eu kinase binding assay and surface plasmon resonance method in elucidating the binding kinetics of focal adhesion kinase inhibitors.

Jennifer L. Mason, C. Spais, T. Angeles, 2012, Assay and drug development technologies.

TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone.

J. Mallamo, T. Angeles, R. Tripathy, 2008, Bioorganic & medicinal chemistry letters.

Enzyme-linked immunosorbent assay for trkA tyrosine kinase activity.

R. Stephens, C. Dionne, D. Kaplan, 1996, Analytical biochemistry.

Sustained in vivo regression of Dunning H rat prostate cancers treated with combinations of androgen ablation and Trk tyrosine kinase inhibitors, CEP-751 (KT-6587) or CEP-701 (KT-5555).

J. Isaacs, C. Murakata, T. Angeles, 1999, Cancer research.

Depletion of Autoreactive Plasma Cells and Treatment of Lupus Nephritis in Mice Using CEP-33779, a Novel, Orally Active, Selective Inhibitor of JAK2

Jennifer L. Mason, P. Dobrzanski, B. Ruggeri, 2011, The Journal of Immunology.

Kinetics of trkA tyrosine kinase activity and inhibition by K-252a.

C. Dionne, T. Angeles, C. Steffler, 1998, Archives of biochemistry and biophysics.

Isoabzymes: structurally and mechanistically similar catalytic antibodies from the same immunization.

P. Schultz, J. Kenten, R. Sanchez, 1993, Biochemistry.

A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clini

B. Ruggeri, J. Mallamo, D. Gingrich, 2003, Journal of medicinal chemistry.

Aspects of antibody-catalyzed primary amide hydrolysis

G. Blackburn, R. Titmas, G. Blackburn, 1994, Applied biochemistry and biotechnology.

CEP-7055: a novel, orally active pan inhibitor of vascular endothelial growth factor receptor tyrosine kinases with potent antiangiogenic activity and antitumor efficacy in preclinical models.

A. Klein-Szanto, P. Casellas, P. Dobrzanski, 2003, Cancer research.

Comparison of two homogeneous cell-based kinase assays for JAK2 V617F: SureFire pSTAT5 and GeneBLAzer fluorescence resonance energy transfer assays.

Jennifer L. Mason, J. Qian, T. Angeles, 2012, Assay and drug development technologies.

TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs.

Allison L. Zulli, B. Ruggeri, T. Underiner, 2008, Bioorganic & medicinal chemistry letters.

Novel C-3 N-urea, amide, and carbamate dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs as potent TIE-2 and VEGF-R2 dual inhibitors.

Allison L. Zulli, Hong Chang, C. Robinson, 2006, Bioorganic & medicinal chemistry letters.

Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells.

B. Ruggeri, T. Underiner, B. Dorsey, 2006, Blood.

Mixed lineage kinase activity of indolocarbazole analogues.

D. Bozyczko‐Coyne, C. Murakata, T. Angeles, 2002, Bioorganic & medicinal chemistry letters.

Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis.

E. Bacon, B. Ruggeri, J. Mallamo, 2006, Bioorganic & medicinal chemistry letters.

Depletion of Autoreactive Plasma Cells and Treatment of Lupus Nephritis in Mice Using CEP-33779, a Novel, Orally Active, Selective Inhibitor of JAK2

Jennifer L. Mason, P. Dobrzanski, B. Ruggeri, 2011, The Journal of Immunology.

Inhibitor of JAK2 CEP-33779, a Novel, Orally Active, Selective Treatment of Lupus Nephritis in Mice Using Depletion of Autoreactive Plasma Cells and

Mason, B. Ruggeri, D. Gingrich, 2011 .

Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).

A. Ghose, P. Dobrzanski, E. Bruckheimer, 2016, Journal of medicinal chemistry.

Time-resolved fluorescence resonance energy transfer as a versatile tool in the development of homogeneous cellular kinase assays.

Jennifer L. Mason, C. Spais, T. Angeles, 2012, Assay and drug development technologies.

Improvement of inhibitor identification for heat shock protein 90α by utilizing a red-shifted fluorescence polarization probe.

T. Underiner, J. Qian, T. Angeles, 2012, Assay and drug development technologies.

Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.

A. Ghose, B. Ruggeri, K. Wells-Knecht, 2012, Journal of medicinal chemistry.

Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a.

J. Mallamo, T. Angeles, R. Hudkins, 2007, Journal of medicinal chemistry.

1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.

A. Ghose, E. Bacon, J. Mallamo, 2007, Bioorganic & medicinal chemistry letters.

Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group.

A. Ghose, B. Dorsey, T. Angeles, 2011, Bioorganic & medicinal chemistry letters.

Design, synthesis, and anaplastic lymphoma kinase (ALK) inhibitory activity for a novel series of 2,4,8,22-tetraazatetracyclo[14.3.1.1³,⁷.1⁹,¹³]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles.

A. Ghose, K. Wells-Knecht, H. Breslin, 2012, Journal of medicinal chemistry.

Design of 7-amino-6-chloro-3H-imidazo[4,5-b]pyridine scaffold from 5-chloro-2,4-diaminopyrimidine pharmacophore: identification of potent inhibitors of anaplastic lymphoma kinase

A. Ghose, B. Dorsey, T. Angeles, 2012 .

A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.

Jennifer L. Mason, Pawel Dobrzanski, Bruce D. Dorsey, 2012, Journal of medicinal chemistry.

Recent advances in targeting the fatty acid biosynthetic pathway using fatty acid synthase inhibitors

T. Angeles, R. Hudkins, 2016, Expert opinion on drug discovery.

2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.

A. Ghose, B. Ruggeri, D. Gingrich, 2011, Journal of medicinal chemistry.

Antibody-Catalyzed Hydrolysis of an Unsubstituted Amide

P. M. Booth, A. Napper, R. Titmas, 1994 .

Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.

Andrew V. Anzalone, B. Ruggeri, T. Underiner, 2010, ACS medicinal chemistry letters.

Reversal of enzyme regiospecificity with alternative substrates for aspartokinase I from Escherichia coli.

R. Viola, T. Angeles, J. Hunsley, 1992, Biochemistry.

The kinetic mechanisms of the bifunctional enzyme aspartokinase-homoserine dehydrogenase I from Escherichia coli.

R. Viola, T. Angeles, 1990, Archives of biochemistry and biophysics.

Aspartokinase-homoserine dehydrogenase I from Escherichia coli: pH and chemical modification studies of the kinase activity.

R. Viola, T. Angeles, C. L. Borders, 1989, Biochemistry.

Use of steady state kinetic methods to elucidate the kinetic and chemical mechanisms of retroviral proteases.

T. Meek, T. Angeles, E. J. Rodriguez, 1994, Methods in enzymology.

Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.

A. Ghose, K. L. Milkiewicz, T. Underiner, 2010, Bioorganic & medicinal chemistry.

Use of nitrogen-15 kinetic isotope effects to elucidate details of the chemical mechanism of human immunodeficiency virus 1 protease.

T. Meek, T D Meek, T. Angeles, 1993, Biochemistry.

Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.

B. Ruggeri, R. Haltiwanger, B. Dorsey, 2015, Bioorganic & medicinal chemistry letters.

Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.

K. Wells-Knecht, H. Breslin, B. Dorsey, 2012, Journal of medicinal chemistry.

CEP-28122, a Highly Potent and Selective Orally Active Inhibitor of Anaplastic Lymphoma Kinase with Antitumor Activity in Experimental Models of Human Cancers

G. Inghirami, B. Ruggeri, D. Gingrich, 2011, Molecular Cancer Therapeutics.

Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.

Andrew V. Anzalone, Jason P. Burke, B. Ruggeri, 2011, Bioorganic & medicinal chemistry letters.

ALK mutants in the kinase domain exhibit altered kinase activity and differential sensitivity to small molecule ALK inhibitors.

A. Ghose, B. Ruggeri, J. T. Durkin, 2009, Biochemistry.

Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.

D. Bozyczko‐Coyne, A. Fedorov, E. Fedorov, 2008, Journal of Medicinal Chemistry.

Phosphoregulation of mixed-lineage kinase 1 activity by multiple phosphorylation in the activation loop.

Karla K Kopec, C. Spais, J. T. Durkin, 2004, Biochemistry.

Motoneuron Apoptosis Is Blocked by CEP-1347 (KT 7515), a Novel Inhibitor of the JNK Signaling Pathway

N. Neff, M. Glicksman, A. Maroney, 1998, The Journal of Neuroscience.

CEP-1347 (KT7515), a Semisynthetic Inhibitor of the Mixed Lineage Kinase Family*

L. Greene, A. Maroney, Zhiheng Xu, 2001, The Journal of Biological Chemistry.

Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]

Allison L. Zulli, E. Bacon, B. Ruggeri, 2012, Journal of medicinal chemistry.

8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors.

A. Fedorov, E. Fedorov, S. Almo, 2010, Bioorganic & medicinal chemistry letters.

A radioactive binding assay for inhibitors of trkA kinase.

C. Dionne, A. Maroney, T. Angeles, 1997, Analytical biochemistry.

A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis

P. Dobrzanski, B. Ruggeri, D. Gingrich, 2011, Arthritis research & therapy.

Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders.

Pawel Dobrzanski, M. Carroll, P. Dobrzanski, 2008, Blood.

Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test.

Karla K Kopec, E. Duzic, E. Bacon, 2012, Bioorganic & medicinal chemistry letters.

CEP-701 Is a JAK2 Inhibitor Which Attenuates JAK2/STAT5 Signaling Pathway and the Proliferation of Primary Cells from Patients with Myeloproliferative Disorders.

M. Carroll, P. Dobrzanski, B. Ruggeri, 2006 .

Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists.

Karla K Kopec, E. Duzic, E. Bacon, 2012, Bioorganic & medicinal chemistry letters.

Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.

T. Underiner, B. Dorsey, T. Angeles, 2011, Bioorganic & medicinal chemistry letters.

Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.

Allison L. Zulli, E. Bacon, B. Ruggeri, 2008, Bioorganic & medicinal chemistry letters.

Neurotrophic 3,9-bis[(alkylthio)methyl]-and-bis(alkoxymethyl)-K-252a derivatives.

N. Neff, M. Glicksman, C. Dionne, 1997, Journal of medicinal chemistry.

Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.

D. Gingrich, T. Angeles, R. Hudkins, 2005, Journal of medicinal chemistry.

Quantitative, high-throughput cell-based assays for inhibitors of trkA receptor.

T. Angeles, J. Lippy, S. X. Yang, 2000, Analytical biochemistry.

Fused pyrrolo[2,3-c]carbazol-6-ones: novel immunostimulants that enhance human interferon-gamma activity.

T. Angeles, R. Hudkins, E. Knight, 1997, Journal of Medicinal Chemistry.

Fused Pyrrolo(2,3-c)carbazol-6-ones: Novel Immunostimulants That Enhance Human Interferon-γ Activity.

T. Angeles, R. Hudkins, E. Knight, 1997 .

2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.

Jennifer L. Mason, K. L. Milkiewicz, K. Wells-Knecht, 2011, Bioorganic & Medicinal Chemistry Letters.

Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.

Jennifer L. Mason, P. Dobrzanski, K. L. Milkiewicz, 2012, Bioorganic & medicinal chemistry letters.

Modification of CellSensor irf1-bla TF-1 and irf1-bla HEL assays for direct comparison of wild-type JAK2 and JAK2 V617F inhibition.

Jennifer L. Mason, K. Wells-Knecht, T. Angeles, 2011, Assay and drug development technologies.

Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.

K. L. Milkiewicz, T. Underiner, B. Dorsey, 2011, Bioorganic & medicinal chemistry letters.

Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.

K. L. Milkiewicz, S. Miknyoczki, T. Underiner, 2011, Bioorganic & medicinal chemistry.

CEP‐751 inhibits trk receptor tyrosine kinase activity in vitro and exhibits anti‐tumor activity

N. Neff, J. Isaacs, A. Maroney, 1997, International journal of cancer.

Solvent isotope partitioning: a new kinetic tool for the determination of desorption rates of reactant water from enzyme-substrate complexes in proteases.

S. Carr, T. Meek, G. Roberts, 1992, Biochemistry.

Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.

R. Haltiwanger, B. Dorsey, T. Angeles, 2015, Bioorganic & medicinal chemistry letters.

A. Ghose, K. Wells-Knecht, H. Breslin, 2012, Journal of medicinal chemistry.