Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40
Lu, Jun, Byrne, Noel, Wang, John, Bricogne, Gerard, Brown, Frank K, Chobanian, Harry R, Colletti, Steven L, Di Salvo, Jerry, Thomas-Fowlkes, Brande, Guo, Yan, Hall, Dawn L, Hadix, Jennifer, Hastings, Nicholas B, Hermes, Jeffrey D, Ho, Thu, Howard, Andrew D, Josien, Hubert, Kornienko, Maria, Lumb, Kevin J, Miller, Michael W, Patel, Sangita B, Pio, Barbara, Plummer, Christopher W, Sherborne, Bradley S, Sheth, Payal, Souza, Sarah, Tummala, Srivanya, Vonrhein, Clemens, Webb, Maria, Allen, Samantha J, Johnston, Jennifer M, Weinglass, Adam B, Sharma, Sujata, Soisson, Stephen M
Published in Nature structural & molecular biology (01.07.2017)
Published in Nature structural & molecular biology (01.07.2017)
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Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists
Chandramohan, Arun, Josien, Hubert, Yuen, Tsz Ying, Duggal, Ruchia, Spiegelberg, Diana, Yan, Lin, Juang, Yu-Chi Angela, Ge, Lan, Aronica, Pietro G, Kaan, Hung Yi Kristal, Lim, Yee Hwee, Peier, Andrea, Sherborne, Brad, Hochman, Jerome, Lin, Songnian, Biswas, Kaustav, Nestor, Marika, Verma, Chandra S, Lane, David P, Sawyer, Tomi K, Garbaccio, Robert, Henry, Brian, Kannan, Srinivasaraghavan, Brown, Christopher J, Johannes, Charles W, Partridge, Anthony W
Published in Nature communications (12.01.2024)
Published in Nature communications (12.01.2024)
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Discovery of a Novel, Potent Spirocyclic Series of γ‑Secretase Inhibitors
Zhao, Zhiqiang, Pissarnitski, Dmitri A, Josien, Hubert B, Wu, Wen-Lian, Xu, Ruo, Li, Hongmei, Clader, John W, Burnett, Duane A, Terracina, Giuseppe, Hyde, Lynn, Lee, Julie, Song, Lixin, Zhang, Lili, Parker, Eric M
Published in Journal of medicinal chemistry (25.11.2015)
Published in Journal of medicinal chemistry (25.11.2015)
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Journal Article
Substituted 4-morpholine N-arylsulfonamides as γ-secretase inhibitors
Zhao, Zhiqiang, Pissarnitski, Dmitri A., Josien, Hubert B., Bara, Thomas A., Clader, John W., Li, Hongmei, McBriar, Mark D., Rajagopalan, Murali, Xu, Ruo, Terracina, Giuseppe, Hyde, Lynn, Song, Lixin, Zhang, Lili, Parker, Eric M., Osterman, Rebecca, Buevich, Alexei V.
Published in European journal of medicinal chemistry (29.11.2016)
Published in European journal of medicinal chemistry (29.11.2016)
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A high-throughput microfluidic mechanoporation platform to enable intracellular delivery of cyclic peptides in cell-based assays
Kasper, Stephen H, Otten, Stephanie, Squadroni, Brian, Orr-Terry, Cionna, Kuang, Yi, Mussallem, Lily, Ge, Lan, Yan, Lin, Kannan, Srinivasaraghavan, Verma, Chandra S, Brown, Christopher J, Johannes, Charles W, Lane, David P, Chandramohan, Arun, Partridge, Anthony W, Roberts, Lee R, Josien, Hubert, Therien, Alex G, Hett, Erik C, Howell, Bonnie J, Peier, Andrea, Ai, Xi, Cassaday, Jason
Published in Bioengineering & translational medicine (01.09.2023)
Published in Bioengineering & translational medicine (01.09.2023)
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Tetrahydroquinoline sulfonamides as γ-secretase inhibitors
Asberom, Theodros, Bara, Thomas A., Clader, John W., Greenlee, William J., Guzik, Henry S., Josien, Hubert B., Li, Wei, Parker, Eric M., Pissarnitski, Dmitri A., Song, Lixin, Zhang, Lili, Zhao, Zhiqiang
Published in Bioorganic & medicinal chemistry letters (2007)
Published in Bioorganic & medicinal chemistry letters (2007)
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Journal Article
Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as γ-secretase inhibitors
Li, Hongmei, Asberom, Theodros, Bara, Thomas A., Clader, John W., Greenlee, William J., Josien, Hubert B., McBriar, Mark D., Nomeir, Amin, Pissarnitski, Dmitri A., Rajagopalan, Murali, Xu, Ruo, Zhao, Zhiqiang, Song, Lixin, Zhang, Lili
Published in Bioorganic & medicinal chemistry (15.11.2007)
Published in Bioorganic & medicinal chemistry (15.11.2007)
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Journal Article
2,6-Disubstituted N-arylsulfonyl piperidines as γ-secretase inhibitors
Pissarnitski, Dmitri A., Asberom, Theodros, Bara, Thomas A., Buevich, Alex V., Clader, John W., Greenlee, William J., Guzik, Henry S., Josien, Hubert B., Li, Wei, McEwan, Michael, McKittrick, Brian A., Nechuta, Terry L., Parker, Eric M., Sinning, Lisa, Smith, Elizabeth M., Song, Lixin, Vaccaro, Henry A., Voigt, Johannes H., Zhang, Lili, Zhang, Qi, Zhao, Zhiqiang
Published in Bioorganic & medicinal chemistry letters (2007)
Published in Bioorganic & medicinal chemistry letters (2007)
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Journal Article
Discovery of γ-secretase inhibitors efficacious in a transgenic animal model of Alzheimer’s disease
Asberom, Theodros, Zhao, Zhiqiang, Bara, Thomas A., Clader, John W., Greenlee, William J., Hyde, Lynn A., Josien, Hubert B., Li, Wei, McPhail, Andrew T., Nomeir, Amin A., Parker, Eric M., Rajagopalan, Murali, Song, Lixin, Wong, Gwendolyn T., Zhang, Lili, Zhang, Qi, Pissarnitski, Dmitri A.
Published in Bioorganic & medicinal chemistry letters (15.01.2007)
Published in Bioorganic & medicinal chemistry letters (15.01.2007)
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SAR of tricyclic sulfones as γ-secretase inhibitors
Xu, Ruo, Cole, David, Asberom, Ted, Bara, Tom, Bennett, Chad, Burnett, Duane A., Clader, John, Domalski, Martin, Greenlee, William J., Hyde, Lynn, Josien, Hubert, Li, HongMei, McBriar, Mark, McKittrick, Brian, Pissarnitski, Dmitri, Qiang, Li, Rajagopalan, Murali, Sasikumar, Thavalakulamgara, Su, Jing, Tang, HaiQun, Wu, Wen-Lian, Zhang, LiLi, Zhao, ZhiQiang
Published in Science China. Chemistry (01.11.2011)
Published in Science China. Chemistry (01.11.2011)
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Concise Formation of 4-Benzyl Piperidines and Related Derivatives Using a Suzuki Protocol
Vice, Susan, Bara, Tom, Bauer, Annette, Evans, C. Anderson, Ford, Jennifer, Josien, Hubert, McCombie, Stuart, Miller, Michael, Nazareno, Dennis, Palani, Anandan, Tagat, Jay
Published in Journal of organic chemistry (06.04.2001)
Published in Journal of organic chemistry (06.04.2001)
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Synthesis of Mono- and Difluoronaphthoic Acids
Tagat, Jayaram R, McCombie, Stuart W, Nazareno, Dennis V, Boyle, Craig D, Kozlowski, Joseph A, Chackalamannil, Samuel, Josien, Hubert, Wang, Yuguang, Zhou, Guowei
Published in Journal of organic chemistry (22.02.2002)
Published in Journal of organic chemistry (22.02.2002)
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Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor
Johns, Douglas G, Campeau, Louis-Charles, Banka, Puja, Bautmans, An, Bueters, Tjerk, Bianchi, Elisabetta, Branca, Danila, Bulger, Paul G, Crevecoeur, Inne, Ding, Fa-Xiang, Garbaccio, Robert M, Guetschow, Erik D, Guo, Yan, Ha, Sookhee N, Johnston, Jennifer M, Josien, Hubert, Kauh, Eunkyung A, Koeplinger, Kenneth A, Kuethe, Jeffrey T, Lai, Eseng, Lanning, Christine L, Lee, Anita Y H, Li, Li, Nair, Anilkumar G, O'Neill, Edward A, Stoch, S Aubrey, Thaisrivongs, David A, Tucker, Thomas J, Vachal, Petr, van Dyck, Kristien, Vanhoutte, Frederic P, Volckaert, Bram, Wolford, Dennis G, Xu, Andy, Zhao, Tian, Zhou, Dan, Zhou, Susan, Zhu, Xiaohong, Zokian, Hratch J, Walji, Abbas M, Wood, Harold B
Published in Circulation (New York, N.Y.) (11.07.2023)
Published in Circulation (New York, N.Y.) (11.07.2023)
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Bioactivation of GPR40 Agonist MK-8666: Formation of Protein Adducts in Vitro from Reactive Acyl Glucuronide and Acyl CoA Thioester
Shang, Jackie, Tschirret-Guth, Richard, Cancilla, Mark, Samuel, Koppara, Chen, Qing, Chobanian, Harry R, Thomas, Ann, Tong, Wei, Josien, Hubert, Buevich, Alexei V, Mitra, Kaushik
Published in Chemical research in toxicology (21.01.2020)
Published in Chemical research in toxicology (21.01.2020)
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Leveraging High-Resolution Ion Mobility-Mass Spectrometry for Cyclic Peptide Soft Spot Identification
Fawaz, Maria, Sun, Congliang, Feng, Yu, Qirjollari, Athanasia, Josien, Hubert, DeBord, Daniel, Simone, Ashli, Williamson, David L, Pearson, Kara, Gonzalez, Raymond J, Vasicek, Lisa, Cancilla, Mark T, Wang, Weixun, Spellman, Daniel S, Kedia, Komal
Published in Journal of the American Society for Mass Spectrometry (11.07.2024)
Published in Journal of the American Society for Mass Spectrometry (11.07.2024)
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Metabolic stabilization of benzylidene ketal M2 muscarinic receptor antagonists via halonaphthoic acid substitution
BOYLE, Craig D, CHACKALAMANNIL, Samuel, YUGUANG WANG, GUOWEI ZHOU, BILLARD, William, BINCH, Herbert III, CROSBY, Gordon, COHEN-WILLIAMS, Mary, COFFIN, Vicki L, COX, Kathleen A, GROTZ, Diane E, DUFFY, Ruth A, CLADER, John W, RUPERTO, Vilma, LACHOWICZ, Jean E, GREENLEE, William J, JOSIEN, Hubert B, KAMINSKI, James J, KOZLOWSKI, Joseph A, MCCOMBIE, Stuart W, NAZARENO, Dennis V, TAGAT, Jayaram R
Published in Bioorganic & medicinal chemistry letters (03.09.2001)
Published in Bioorganic & medicinal chemistry letters (03.09.2001)
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Journal Article
Design-Rules for Stapled Alpha-Helical Peptides with On-Target In Vivo Activity: Application to Mdm2/X dual antagonists
Chandramohan, Arun, Josien, Hubert, Yuen, Tsz Ying, Duggal, Ruchia, Spiegelberg, Diana, Yan, Lin, Angela Juang, Yu-Chi, Ge, Lan, Aronica, Pietro, Kaan, Kristal, Lim, Yee Hwee, Peier, Andrea, Sherborne, Brad, Hochman, Jerome, Lin, Songnian, Biswas, Kaustav, Henry, Brian, Nestor, Marika, Verma, Chandra S, Lane, David, Sawyer, Tomi, Garbaccio, Robert, Kannan, Srinivasaraghavan, Brown, Christopher J., Johannes, Charles W, Partridge, Anthony William
Published in Nature communications (26.02.2023)
Published in Nature communications (26.02.2023)
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Journal Article
Chronic Treatment with the γ-Secretase Inhibitor LY-411,575 Inhibits β-Amyloid Peptide Production and Alters Lymphopoiesis and Intestinal Cell Differentiation
Wong, Gwendolyn T., Manfra, Denise, Poulet, Frederique M., Zhang, Qi, Josien, Hubert, Bara, Thomas, Engstrom, Laura, Pinzon-Ortiz, Maria, Fine, Jay S., Lee, Hu-Jung J., Zhang, Lili, Higgins, Guy A., Parker, Eric M.
Published in The Journal of biological chemistry (26.03.2004)
Published in The Journal of biological chemistry (26.03.2004)
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