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
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)
Published in Journal of medicinal chemistry (28.07.2016)
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Structure-Based Design of Selective LONP1 Inhibitors for Probing In Vitro Biology
Kingsley, Laura J, He, Xiaohui, McNeill, Matthew, Nelson, John, Nikulin, Victor, Ma, Zhiwei, Lu, Wenshuo, Zhou, Vicki W, Manuia, Mari, Kreusch, Andreas, Gao, Mu-Yun, Witmer, Darbi, Vaillancourt, Mei-Ting, Lu, Min, Greenblatt, Sarah, Lee, Christian, Vashisht, Ajay, Bender, Steven, Spraggon, Glen, Michellys, Pierre-Yves, Jia, Yong, Haling, Jacob R, Lelais, Gérald
Published in Journal of medicinal chemistry (22.04.2021)
Published in Journal of medicinal chemistry (22.04.2021)
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EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor
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)
Published in Cancer research (Chicago, Ill.) (15.03.2016)
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Integrating pharmacokinetic-pharmacodynamic modeling in preclinical assessment of mutant selective EGFR covalent tyrosine kinase inhibitor EGF816
Li, Chun, Jia, Yong, Lelais, Gerald, Li, Jie, Shapiro, Michael, Groessl, Todd, Vaillancourt, Mei-Ting, Tompkins, Celin, Tuntland, Tove, Isbell, John, Bender, Steve, Cui, Xiaoming
Published in Drug metabolism and pharmacokinetics (01.01.2019)
Published in Drug metabolism and pharmacokinetics (01.01.2019)
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Discovery of ( R , E )- N -(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1 H -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
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)
Published in Journal of medicinal chemistry (28.07.2016)
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Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors
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)
Published in Nature (London) (02.06.2016)
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Development of a virtual reality platform for effective communication of structural data in drug discovery
Kingsley, Laura J., Brunet, Vincent, Lelais, Gerald, McCloskey, Steve, Milliken, Kelly, Leija, Edgardo, Fuhs, Stephen R., Wang, Kai, Zhou, Edward, Spraggon, Glen
Published in Journal of molecular graphics & modelling (01.06.2019)
Published in Journal of molecular graphics & modelling (01.06.2019)
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beta-Peptidic secondary structures fortified and enforced by Zn2+ complexation - On the way to beta-peptidic zinc fingers?
Lelais, G, Seebach, D, Jaun, B, Mathad, RI, Flogel, O, Rossi, F, Campo, M, Wortmann, A
Published in Helvetica chimica acta (01.03.2006)
Published in Helvetica chimica acta (01.03.2006)
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Dexamethasone inhibits respiratory syncytial virus-driven mucus production while increasing viral replication without altering antiviral interferon signaling
McAllister, Christopher S., Ansaldi, Dan, Growcott, Ellena J., Zhong, Yang, Quackenbush, Doug, Wolff, Karen C., Chen, Zhong, Tanaseichuk, Olga, Lelais, Gerald, Barnes, S. Whitney, Federe, Glenn C., Luna, Fabio, Walker, John R., Zhou, Yingyao, Kuhen, Kelli L.
Published in Virology (New York, N.Y.) (15.01.2020)
Published in Virology (New York, N.Y.) (15.01.2020)
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