Search Results - "Thomas H. Marsilje" :: K.UTB vyhledávací portál | TBU Library Retrieval Portal

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

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

by Jia, Yong, Juarez, Jose, Li, Jie, Manuia, Mari, Niederst, Matthew J, Tompkins, Celin, Timple, Noelito, Vaillancourt, Mei-Ting, Pferdekamper, AnneMarie Culazzo, Lockerman, Elizabeth L, Li, Chun, Anderson, Jennifer, Costa, Carlotta, Liao, Debbie, Murphy, Eric, DiDonato, Michael, Bursulaya, Badry, Lelais, Gerald, Barretina, Jordi, McNeill, Matthew, Epple, Robert, Marsilje, Thomas H, Pathan, Nuzhat, Engelman, Jeffrey A, Michellys, Pierre-Yves, McNamara, Peter, Harris, Jennifer, Bender, Steven, Kasibhatla, Shailaja
Published in Cancer research (Chicago, Ill.) (15.03.2016)

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

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

by Jia, Yong, Yun, Cai-Hong, Park, Eunyoung, Ercan, Dalia, Manuia, Mari, Juarez, Jose, Xu, Chunxiao, Rhee, Kevin, Chen, Ting, Zhang, Haikuo, Palakurthi, Sangeetha, Jang, Jaebong, Lelais, Gerald, DiDonato, Michael, Bursulaya, Badry, Michellys, Pierre-Yves, Epple, Robert, Marsilje, Thomas H., McNeill, Matthew, Lu, Wenshuo, Harris, Jennifer, Bender, Steven, Wong, Kwok-Kin, Jänne, Pasi A., Eck, Michael J.
Published in Nature (London) (02.06.2016)

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

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

by Kim, Min-Ju, Park, Sang Ho, Opella, Stanley J., Marsilje, Thomas H., Michellys, Pierre-Yves, Seidel, H. Martin, Tian, Shin-Shay
Published in The Journal of biological chemistry (11.05.2007)

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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 Clinical Trials

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 Clinical Trials

by Marsilje, Thomas H, Pei, Wei, Chen, Bei, Lu, Wenshuo, Uno, Tetsuo, Jin, Yunho, Jiang, Tao, Kim, Sungjoon, Li, Nanxin, Warmuth, Markus, Sarkisova, Yelena, Sun, Frank, Steffy, Auzon, Pferdekamper, AnneMarie C, Li, Allen G, Joseph, Sean B, Kim, Young, Liu, Bo, Tuntland, Tove, Cui, Xiaoming, Gray, Nathanael S, Steensma, Ruo, Wan, Yongqin, Jiang, Jiqing, Chopiuk, Greg, Li, Jie, Gordon, W. Perry, Richmond, Wendy, Johnson, Kevin, Chang, Jonathan, Groessl, Todd, He, You-Qun, Phimister, Andrew, Aycinena, Alex, Lee, Christian C, Bursulaya, Badry, Karanewsky, Donald S, Seidel, H. Martin, Harris, Jennifer L, Michellys, Pierre-Yves
Published in Journal of medicinal chemistry (25.07.2013)

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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-Cell Lung Cancers

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-Cell Lung Cancers

by Lelais, Gérald, Epple, Robert, Marsilje, Thomas H, Long, Yun O, McNeill, Matthew, Chen, Bei, Lu, Wenshuo, Anumolu, Jaganmohan, Badiger, Sangamesh, Bursulaya, Badry, DiDonato, Michael, Fong, Rina, Juarez, Jose, Li, Jie, Manuia, Mari, Mason, Daniel E, Gordon, Perry, Groessl, Todd, Johnson, Kevin, Jia, Yong, Kasibhatla, Shailaja, Li, Chun, Isbell, John, Spraggon, Glen, Bender, Steven, Michellys, Pierre-Yves
Published in Journal of medicinal chemistry (28.07.2016)

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

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

by Alper, Phil B., Marsilje, Thomas H., Mutnick, Daniel, Lu, Wenshuo, Chatterjee, Arnab, Roberts, Michael J., He, Yun, Karanewsky, Donald S., Chow, Donald, Lao, Jianmin, Gerken, Andrea, Tuntland, Tove, Liu, Bo, Chang, Jonathan, Gordon, Perry, Martin Seidel, H., Tian, Shin-Shay
Published in Bioorganic & medicinal chemistry (01.10.2008)

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Identification and Characterization of Small Molecule Modulators of the Epstein–Barr Virus-Induced Gene 2 (EBI2) Receptor

Identification and Characterization of Small Molecule Modulators of the Epstein–Barr Virus-Induced Gene 2 (EBI2) Receptor

by Gessier, Francois, Preuss, Inga, Yin, Hong, Rosenkilde, Mette M, Laurent, Stephane, Endres, Ralf, Chen, Yu A, Marsilje, Thomas H, Seuwen, Klaus, Nguyen, Deborah G, Sailer, Andreas W
Published in Journal of medicinal chemistry (24.04.2014)

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A Blueprint to Advance Colorectal Cancer Immunotherapies

A Blueprint to Advance Colorectal Cancer Immunotherapies

by Le, Dung T, Hubbard-Lucey, Vanessa M, Morse, Michael A, Heery, Christopher R, Dwyer, Andrea, Marsilje, Thomas H, Brodsky, Arthur N, Chan, Emily, Deming, Dustin A, Diaz, Jr, Luis A, Fridman, Wolf H, Goldberg, Richard M, Hamilton, Stanley R, Housseau, Franck, Jaffee, Elizabeth M, Kang, S Peter, Krishnamurthi, Smitha S, Lieu, Christopher H, Messersmith, Wells, Sears, Cynthia L, Segal, Neil H, Yang, Arvin, Moss, Rebecca A, Cha, Edward, O'Donnell-Tormey, Jill, Roach, Nancy, Davis, Anjelica Q, McAbee, Keavy, Worrall, Sharyn, Benson, Al B
Published in Cancer immunology research (01.11.2017)

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

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

by MARSILJE, Thomas H, ROSES, Jonathan B, DANIELS, J. Scott, PING LI, LIJUN WU, PATANE, Michael A, CLAIBORNE, Christopher F, CALDERWOOD, Emily F, STROUD, Stephen G, FORSYTH, Nancy E, BLACKBURN, Christopher, YOWE, David L, MIAO, Wenyan, DRABIC, Stacey V, BOHANE, Marie D
Published in Bioorganic & medicinal chemistry letters (16.07.2004)

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

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

by Greasley, Samantha E, Marsilje, Thomas H, Cai, Hui, Baker, Stephen, Benkovic, Stephen J, Boger, Dale L, Wilson, Ian A
Published in Biochemistry (Easton) (13.11.2001)

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Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors

Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors

by Michellys, Pierre-Yves, Chen, Bei, Jiang, Tao, Jin, Yunho, Lu, Wenshuo, Marsilje, Thomas H., Pei, Wei, Uno, Tetsuo, Zhu, Xuefeng, Wu, Baogen, Nguyen, Truc Ngoc, Bursulaya, Badry, Lee, Christian, Li, Nanxin, Kim, Sungjoon, Tuntland, Tove, Liu, Bo, Sun, Frank, Steffy, Auzon, Hood, Tami
Published in Bioorganic & medicinal chemistry letters (01.02.2016)

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

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

by Fairhurst, Robin A., Marsilje, Thomas H., Stutz, Stefan, Boos, Andreas, Niklaus, Michel, Chen, Bei, Jiang, Songchun, Lu, Wenshuo, Furet, Pascal, McCarthy, Clive, Stauffer, Frédéric, Guagnano, Vito, Vaupel, Andrea, Michellys, Pierre-Yves, Schnell, Christian, Jeay, Sébastien
Published in Bioorganic & medicinal chemistry letters (15.04.2016)

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High-Content Micronucleus Assay in Genotoxicity Profiling: Initial-Stage Development and Some Applications in the Investigative/Lead-Finding Studies in Drug Discovery

High-Content Micronucleus Assay in Genotoxicity Profiling: Initial-Stage Development and Some Applications in the Investigative/Lead-Finding Studies in Drug Discovery

by Mondal, Madhu S., Gabriels, Joseph, McGinnis, Claudia, Magnifico, Maria, Marsilje, Thomas H., Urban, Laszlo, Collis, Alan, Bojanic, Dejan, Biller, Scott A., Frieauff, Wilfried, Martus, Hans-Joerg, Suter, Willi, Bentley, Philip
Published in Toxicological sciences (01.11.2010)

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

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

by Marsilje, Thomas H., Alper, Phil B., Lu, Wenshuo, Mutnick, Daniel, Michellys, Pierre-Yves, He, Yun, Karanewsky, Donald S., Chow, Donald, Gerken, Andrea, Lao, Jianmin, Kim, Min-Ju, Seidel, H. Martin, Tian, Shin-Shay
Published in Bioorganic & medicinal chemistry (01.10.2008)

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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

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

by Zhang, Yan, Desharnais, Joel, Marsilje, Thomas H., Li, Chenglong, Hedrick, Michael P., Gooljarsingh, Lata T., Tavassoli, Ali, Benkovic, Stephen J., Olson, Arthur J., Boger, Dale L., Wilson, Ian A.
Published in Biochemistry (Easton) (27.05.2003)

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

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

by Marsilje, Thomas H, Hedrick, Michael P, Desharnais, Joel, Tavassoli, Ali, Zhang, Yan, Wilson, Ian A, Benkovic, Stephen J, Boger, Dale L
Published in Bioorganic & medicinal chemistry (01.10.2003)

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Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists

Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists

by Vasudevan, Anil, LaMarche, Matthew J., Blackburn, Christopher, Che, Jennifer Lee, Luchaco-Cullis, Courtney A., Lai, Sujen, Marsilje, Thomas H., Patane, Michael A., Souers, Andrew J., Wodka, Derek, Geddes, Bradley, Chen, Sumiao, Brodjian, Seven, Falls, Doug H., Dayton, Brian D., Bush, Eugene, Brune, Michael, Shapiro, Robin D., Marsh, Kennan C., Hernandez, Lisa E., Sham, Hing L., Collins, Christine A., Kym, Philip R.
Published in Bioorganic & medicinal chemistry letters (01.10.2005)

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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

by Marsilje, Thomas H., Pei, Wei, Chen, Bei, Lu, Wenshuo, Uno, Tetsuo, Jin, Yunho, Jiang, Tao, Kim, Sungjoon, Li, Nanxin, Warmuth, Markus, Sarkisova, Yelena, Sun, Frank, Steffy, Auzon, Pferdekamper, AnneMarie C., Li, Allen G., Joseph, Sean B., Kim, Young, Liu, Bo, Tuntland, Tove, Cui, Xiaoming, Gray, Nathanael S., Steensma, Ruo, Wan, Yongqin, Jiang, Jiqing, Chopiuk, Greg, Li, Jie, Gordon, W. Perry, Richmond, Wendy, Johnson, Kevin, Chang, Jonathan, Groessl, Todd, He, You-Qun, Phimister, Andrew, Aycinena, Alex, Lee, Christian C., Bursulaya, Badry, Karanewsky, Donald S., Seidel, H. Martin, Harris, Jennifer L., Michellys, Pierre-Yves
Published in Journal of medicinal chemistry (25.07.2013)

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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

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

by MARSILJE, Thomas H, LABROLI, Marc A, WILSON, Ian A, BEARDSLEY, G. Peter, BENKOVIC, Stephen J, BOGER, Dale L, HEDRICK, Michael P, QING JIN, DESHARNAIS, Joel, BAKER, Stephen J, GOOLJARSINGH, Lata T, RAMCHARAN, Joseph, TAVASSOLI, Ali, YAN ZHANG
Published in Bioorganic & medicinal chemistry (01.08.2002)

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

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

by Marsilje, Thomas H, Hedrick, Michael P, Desharnais, Joel, Capps, Kevin, Tavassoli, Ali, Zhang, Yan, Wilson, Ian A, Benkovic, Stephen J, Boger, Dale L
Published in Bioorganic & medicinal chemistry (01.10.2003)

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