T. Marsilje

发表

Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.

M. Maguire, Courtney A. Cullis, C. Blackburn, 2006, Bioorganic & medicinal chemistry letters.

Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor.

M. Rosenkilde, K. Seuwen, A. Sailer, 2014, Journal of medicinal chemistry.

Unexpected formation of an epoxide-derived multisubstrate adduct inhibitor on the active site of GAR transformylase.

D. Boger, I. Wilson, S. Benkovic, 2001, Biochemistry.

Unexpected Formation of an Epoxide Derived Multisubstrate Adduct Inhibitor on the Active Site of GAR Transformylase

D. Boger, I. Wilson, S. Benkovic, 2001 .

NMR Structural Studies of Interactions of a Small, Nonpeptidyl Tpo Mimic with the Thrombopoietin Receptor Extracellular Juxtamembrane and Transmembrane Domains*

S. Opella, S. H. Park, T. Marsilje, 2007, Journal of Biological Chemistry.

10-Formyl-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid (10-formyl-DDACTHF): a potent cytotoxic agent acting by selective inhibition of human GAR Tfase and the de novo purine biosynthetic pathway.

D. Boger, I. Wilson, S. Benkovic, 2002, Bioorganic & medicinal chemistry.

Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold.

J. Lao, D. Chow, T. Marsilje, 2008, Bioorganic & medicinal chemistry letters.

Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.

J. Lao, A. Chatterjee, T. Tuntland, 2008, Bioorganic & medicinal chemistry letters.

Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.

Thomas Fey, Robin Shapiro, Ju Gao, 2005, Journal of medicinal chemistry.

Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase.

J. H. Shim, D. Boger, S. Benkovic, 2000, Bioorganic & medicinal chemistry.

Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Ce

Chun Xing Li, S. Bender, G. Spraggon, 2016, Journal of medicinal chemistry.

Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.

D. Boger, I. Wilson, S. Benkovic, 2003, Bioorganic & medicinal chemistry.

10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase.

D. Boger, I. Wilson, S. Benkovic, 2003, Bioorganic & medicinal chemistry.

Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid.

Stephen J Benkovic, Yan Zhang, Ali Tavassoli, 2003, Biochemistry.

Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.

J. H. Shim, D. Boger, S. Benkovic, 2000, Bioorganic & medicinal chemistry letters.

Overcoming EGFR T790M and C797S resistance with mutant-selective allosteric inhibitors

Haikuo Zhang, Gerald Lelais, Kwok-Kin Wong, 2016 .

EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.

J. Barretina, Jennifer L. Harris, J. Engelman, 2016, Cancer research.

A Blueprint to Advance Colorectal Cancer Immunotherapies

Vanessa M. Hubbard-Lucey, L. Diaz, E. Jaffee, 2017, Cancer Immunology Research.

The design, synthesis and activity of pentapeptide pp60c-src inhibitors containing L-phosphotyrosine mimics.

J. Lai, D. Hangauer, S. Nair, 2009, The journal of peptide research : official journal of the American Peptide Society.

Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.

Sungjoon Kim, Nanxin Li, Christian C. Lee, 2016, Bioorganic & medicinal chemistry letters.

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2

Sungjoon Kim, Nanxin Li, M. Warmuth, 2013, Journal of medicinal chemistry.

The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives.

K. L. Milkiewicz, M. Hangauer, D. Hangauer, 2000, Bioorganic & medicinal chemistry letters.

The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 1: hydroxynaphthalene derivatives.

K. L. Milkiewicz, D. Hangauer, T. Marsilje, 2000, Bioorganic & medicinal chemistry letters.

Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.

Anil Vasudevan, Christopher Blackburn, A. Vasudevan, 2005, Bioorganic & medicinal chemistry letters.

High-content micronucleus assay in genotoxicity profiling: initial-stage development and some applications in the investigative/lead-finding studies in drug discovery.

Dejan Bojanic, Wilfried Frieauff, D. Bojanic, 2010, Toxicological sciences : an official journal of the Society of Toxicology.

Abstract 2585: Discovery of a potent covalent mutant-selective EGFR inhibitor - the journey from high throughput screening to EGF816

C. Li, S. Kasibhatla, I. Matushansky, 2015 .

Abstract 1734:In vitrocharacterization of EGF816, a third-generation mutant-selective EGFR inhibitor

Jennifer L. Harris, S. Bender, N. Pathan, 2014 .

Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).

Ping Li, Christopher Blackburn, C. Claiborne, 2004, Bioorganic & medicinal chemistry letters.

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

C. Schnell, P. Furet, S. Jeay, 2016, Bioorganic & medicinal chemistry letters.

Overcoming EGFR T790M and C797S resistance with mutant-selective allosteric inhibitors

P. Jänne, Jennifer L. Harris, M. Eck, 2016, Nature.