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)‑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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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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Journal Article
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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Electrophilic S-Trifluoromethylation of Cysteine Side Chains in alpha- and beta-Peptides: Isolation of Trifluoronethylated Sandostatin (R) (Octreotide) Derivatives
Capone, Stefania, Kieltsch, Iris, Floegel, Oliver, Lelais, Gerald, Togni, Antonio, Seebach, Dieter
Published in Helvetica chimica acta (01.01.2008)
Published in Helvetica chimica acta (01.01.2008)
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Abstract 2585: Discovery of a potent covalent mutant-selective EGFR inhibitor - the journey from high throughput screening to EGF816
Lelais, Gerald, Epple, Robert, Michellys, Pierre-Yves, Marsilje, Thomas H., Long, Yun, McNeill, Matthew, Chen, Bei, Lu, Wenshuo, Bursulaya, Badry, DiDonato, Michael, Jia, Yong, Kasibhatla, Shailaja, Li, Chun, Matushansky, Igor, Bender, Steven
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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Journal Article
Overcoming EGFR 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, Janne, Pasi A, Eck, Michael J
Published in Nature (London) (02.06.2016)
Published in Nature (London) (02.06.2016)
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Journal Article
Overcoming EGFR T790M and 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) (25.05.2016)
Published in Nature (London) (25.05.2016)
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Journal Article
Abstract 1733: EGF816, a novel covalent inhibitor of mutant-selective epidermal growth factor receptor, overcomes T790M-mediated resistance in NSCLC
Kasibhatla, Shailaja, Li, Jie, Tompkins, Celin, Vaillancourt, Mei-Ting, Anderson, Jennifer, Pferdekamper, AnneMarie Culazzo, Li, Chun, Long, Oliver, McNeill, Mathew, Epple, Robert, Liao, Debbie, Murphy, Eric, Bender, Steve, Jia, Yong, Lelais, Gerald
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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Abstract 1734: In vitro characterization of EGF816, a third-generation mutant-selective EGFR inhibitor
Jia, Yong, Juarez, Jose, Manuia, Mari, Lelais, Gerald, Kasibhatla, Shailaja, Long, Oliver, McNeill, Matthew, DiDonato, Michael, Bursulaya, Badry, Liao, Debbie, Murphy, Eric, Epple, Robert, Marsilje, Thomas, Pathan, Nuzhat, Michellys, Pierre-Yves, Bender, Steven, Harris, Jennifer
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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Journal Article
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists
Azimioara, Mihai, Alper, Phil, Cow, Christopher, Mutnick, Daniel, Nikulin, Victor, Lelais, Gerald, Mecom, John, McNeill, Matthew, Michellys, Pierre-Yves, Wang, Zhiliang, Reding, Esther, Paliotti, Michael, Li, Jing, Bao, Dingjiu, Zoll, Jocelyn, Kim, Young, Zimmerman, Matthew, Groessl, Todd, Tuntland, Tove, Joseph, Sean B., McNamara, Peter, Seidel, H. Martin, Epple, Robert
Published in Bioorganic & medicinal chemistry letters (01.12.2014)
Published in Bioorganic & medicinal chemistry letters (01.12.2014)
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Journal Article
Electrophilic S-Trifluoromethylation of Cysteine Side Chains in α- and β-Peptides: Isolation of Trifluoro-methylated Sandostatin® (Octreotide) Derivatives
Capone, Stefania, Kieltsch, Iris, Flögel, Oliver, Lelais, Gerald, Togni, Antonio, Seebach, Dieter
Published in Helvetica chimica acta (01.11.2008)
Published in Helvetica chimica acta (01.11.2008)
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Journal Article