Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex
Bussiere, Dirksen E., Xie, Lili, Srinivas, Honnappa, Shu, Wei, Burke, Ashley, Be, Celine, Zhao, Junping, Godbole, Adarsh, King, Dan, Karki, Rajeshri G., Hornak, Viktor, Xu, Fangmin, Cobb, Jennifer, Carte, Nathalie, Frank, Andreas O., Frommlet, Alexandra, Graff, Patrick, Knapp, Mark, Fazal, Aleem, Okram, Barun, Jiang, Songchun, Michellys, Pierre-Yves, Beckwith, Rohan, Voshol, Hans, Wiesmann, Christian, Solomon, Jonathan M., Paulk, Joshiawa
Published in Nature chemical biology (01.01.2020)
Published in Nature chemical biology (01.01.2020)
Get full text
Journal Article
The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer
Friboulet, Luc, Li, Nanxin, Katayama, Ryohei, Lee, Christian C, Gainor, Justin F, Crystal, Adam S, Michellys, Pierre-Yves, Awad, Mark M, Yanagitani, Noriko, Kim, Sungjoon, Pferdekamper, AnneMarie C, Li, Jie, Kasibhatla, Shailaja, Sun, Frank, Sun, Xiuying, Hua, Su, McNamara, Peter, Mahmood, Sidra, Lockerman, Elizabeth L, Fujita, Naoya, Nishio, Makoto, Harris, Jennifer L, Shaw, Alice T, Engelman, Jeffrey A
Published in Cancer discovery (01.06.2014)
Published in Cancer discovery (01.06.2014)
Get full text
Journal Article
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)
Get full text
Journal Article
Target-Based Identification and Optimization of 5‑Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay
Knoepfel, Thomas, Nimsgern, Pierre, Jacquier, Sébastien, Bourrel, Marjorie, Vangrevelinghe, Eric, Glatthar, Ralf, Behnke, Dirk, Alper, Phil B, Michellys, Pierre-Yves, Deane, Jonathan, Junt, Tobias, Zipfel, Géraldine, Limonta, Sarah, Hawtin, Stuart, Andre, Cedric, Boulay, Thomas, Loetscher, Pius, Faller, Michael, Blank, Jutta, Feifel, Roland, Betschart, Claudia
Published in Journal of medicinal chemistry (13.08.2020)
Published in Journal of medicinal chemistry (13.08.2020)
Get full text
Journal Article
Crystal structure of the ALK (anaplastic lymphoma kinase) catalytic domain
Lee, Christian C, Jia, Yong, Li, Nanxin, Sun, Xiuying, Ng, Kenneth, Ambing, Eileen, Gao, Mu-Yun, Hua, Su, Chen, Connie, Kim, Sungjoon, Michellys, Pierre-Yves, Lesley, Scott A, Harris, Jennifer L, Spraggon, Glen
Published in Biochemical journal (15.09.2010)
Published in Biochemical journal (15.09.2010)
Get more information
Journal Article
Author Correction: Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex
Bussiere, Dirksen E., Xie, Lili, Srinivas, Honnappa, Shu, Wei, Burke, Ashley, Be, Celine, Zhao, Junping, Godbole, Adarsh, King, Dan, Karki, Rajeshri G., Hornak, Viktor, Xu, Fangmin, Cobb, Jennifer, Carte, Nathalie, Frank, Andreas O., Frommlet, Alexandra, Graff, Patrick, Knapp, Mark, Fazal, Aleem, Okram, Barun, Jiang, Songchun, Michellys, Pierre-Yves, Beckwith, Rohan, Voshol, Hans, Wiesmann, Christian, Solomon, Jonathan M., Paulk, Joshiawa
Published in Nature chemical biology (01.03.2020)
Published in Nature chemical biology (01.03.2020)
Get full text
Journal Article
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)
Get full text
Journal Article
NMR Structural Studies of Interactions of a Small, Nonpeptidyl Tpo Mimic with the Thrombopoietin Receptor Extracellular Juxtamembrane and Transmembrane Domains
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)
Published in The Journal of biological chemistry (11.05.2007)
Get full text
Journal Article
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
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)
Published in Journal of medicinal chemistry (25.07.2013)
Get full text
Journal Article
Biological Characterization of a Heterodimer-Selective Retinoid X Receptor Modulator: Potential Benefits for the Treatment of Type 2 Diabetes
Leibowitz, Mark D, Ardecky, Robert J, Boehm, Marcus F, Broderick, Carol L, Carfagna, Mark A, Crombie, Diane L, D’Arrigo, Jennifer, Etgen, Garrett J, Faul, Margaret M, Grese, Timothy A, Havel, Henry, Hein, Nancy I, Heyman, Richard A, Jolley, Diane, Klausing, Kay, Liu, Sha, Mais, Dale E, Mapes, Christopher M, Marschke, Keith B, Michellys, Pierre-Yves, Montrose-Rafizadeh, Chahrzad, Ogilvie, Kathleen M, Pascual, Bernadette, Rungta, Deepa, Tyhonas, John S, Urcan, Mary S, Wardlow, Marilyn, Yumibe, Nathan, Reifel-Miller, Anne
Published in Endocrinology (Philadelphia) (01.02.2006)
Published in Endocrinology (Philadelphia) (01.02.2006)
Get full text
Journal Article
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)
Get full text
Journal Article
Discovery of small molecules that target a tertiary-structured RNA
Menichelli, Elena, Lam, Bianca J, Wang, Yu, Wang, Vivian S, Shaffer, Jennifer, Tjhung, Katrina F, Bursulaya, Badry, Nguyen, Truc Ngoc, Vo, Todd, Alper, Phillip B, McAllister, Christopher S, Jones, David H, Spraggon, Glen, Michellys, Pierre-Yves, Joslin, John, Joyce, Gerald F, Rogers, Jeff
Published in Proceedings of the National Academy of Sciences - PNAS (29.11.2022)
Published in Proceedings of the National Academy of Sciences - PNAS (29.11.2022)
Get full text
Journal Article
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)
Get full text
Journal Article
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway
Alper, Phil B., Deane, Jonathan, Betschart, Claudia, Buffet, David, Collignon Zipfel, Géraldine, Gordon, Perry, Hampton, Janice, Hawtin, Stuart, Ibanez, Maureen, Jiang, Tao, Junt, Tobias, Knoepfel, Thomas, Liu, Bo, Maginnis, Jillian, McKeever, Una, Michellys, Pierre-Yves, Mutnick, Daniel, Nayak, Bishnu, Niwa, Satoru, Richmond, Wendy, Rush, James S., Syka, Peter, Zhang, Yi, Zhu, Xuefeng
Published in Bioorganic & medicinal chemistry letters (01.09.2020)
Published in Bioorganic & medicinal chemistry letters (01.09.2020)
Get full text
Journal Article
Discovery of the TLR7/8 Antagonist MHV370 for Treatment of Systemic Autoimmune Diseases
Alper, Phil, Betschart, Claudia, André, Cédric, Boulay, Thomas, Cheng, Dai, Deane, Jonathan, Faller, Michael, Feifel, Roland, Glatthar, Ralf, Han, Dong, Hemmig, Rene, Jiang, Tao, Knoepfel, Thomas, Maginnis, Jillian, Mutnick, Daniel, Pei, Wei, Ruzzante, Giulia, Syka, Peter, Zhang, Guobao, Zhang, Yi, Zink, Florence, Zipfel, Géraldine, Hawtin, Stuart, Junt, Tobias, Michellys, Pierre-Yves
Published in ACS medicinal chemistry letters (10.08.2023)
Published in ACS medicinal chemistry letters (10.08.2023)
Get full text
Journal Article
Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases
He, Xiaohui, Da Ros, Sara, Nelson, John, Zhu, Xuefeng, Jiang, Tao, Okram, Barun, Jiang, Songchun, Michellys, Pierre-Yves, Iskandar, Maya, Espinola, Sheryll, Jia, Yong, Bursulaya, Badry, Kreusch, Andreas, Gao, Mu-Yun, Spraggon, Glen, Baaten, Janine, Clemmer, Leah, Meeusen, Shelly, Huang, David, Hill, Robert, Nguyen-Tran, Vân, Fathman, John, Liu, Bo, Tuntland, Tove, Gordon, Perry, Hollenbeck, Thomas, Ng, Kenneth, Shi, Jian, Bordone, Laura, Liu, Hong
Published in ACS medicinal chemistry letters (12.10.2017)
Published in ACS medicinal chemistry letters (12.10.2017)
Get full text
Journal Article
Design, Synthesis, and Structure−Activity Relationship Studies of Novel 6,7-Locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic Acids
Michellys, Pierre-Yves, Ardecky, Robert J, Chen, Jyun-Hung, D'Arrigo, Jennifer, Grese, Timothy A, Karanewsky, Donald S, Leibowitz, Mark D, Liu, Sha, Mais, Dale A, Mapes, Christopher M, Montrose-Rafizadeh, Chahrzad, Ogilvie, Katheen M, Reifel-Miller, Anne, Rungta, Deepa, Thompson, Anthony W, Tyhonas, John S, Boehm, Marcus F
Published in Journal of medicinal chemistry (11.09.2003)
Published in Journal of medicinal chemistry (11.09.2003)
Get full text
Journal Article
Design, synthesis and structure–activity relationship of novel RXR-selective modulators
Michellys, Pierre-Yves, D'Arrigo, Jennifer, Grese, Timothy A., Karanewsky, Donald S., Leibowitz, Mark D., Mais, Dale A., Mapes, Christopher M., Reifel-Miller, Anne, Rungta, Deepa, Boehm, Marcus F.
Published in Bioorganic & medicinal chemistry letters (22.03.2004)
Published in Bioorganic & medicinal chemistry letters (22.03.2004)
Get full text
Journal Article
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors
Velcicky, Juraj, Mathison, Casey J. N, Nikulin, Victor, Pflieger, Daniel, Epple, Robert, Azimioara, Mihai, Cow, Christopher, Michellys, Pierre-Yves, Rigollier, Pascal, Beisner, Daniel R, Bodendorf, Ursula, Guerini, Danilo, Liu, Bo, Wen, Ben, Zaharevitz, Samantha, Brandl, Trixi
Published in ACS medicinal chemistry letters (13.06.2019)
Published in ACS medicinal chemistry letters (13.06.2019)
Get full text
Journal Article
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors
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)
Published in Bioorganic & medicinal chemistry letters (01.02.2016)
Get full text
Journal Article