A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment
Balestrini, Alessia, Joseph, Victory, Dourado, Michelle, Reese, Rebecca M, Shields, Shannon D, Rougé, Lionel, Bravo, Daniel D, Chernov-Rogan, Tania, Austin, Cary D, Chen, Huifen, Wang, Lan, Villemure, Elisia, Shore, Daniel G M, Verma, Vishal A, Hu, Baihua, Chen, Yong, Leong, Laurie, Bjornson, Chris, Hötzel, Kathy, Gogineni, Alvin, Lee, Wyne P, Suto, Eric, Wu, Xiumin, Liu, John, Zhang, Juan, Gandham, Vineela, Wang, Jianyong, Payandeh, Jian, Ciferri, Claudio, Estevez, Alberto, Arthur, Christopher P, Kortmann, Jens, Wong, Ryan L, Heredia, Jose E, Doerr, Jonas, Jung, Min, Vander Heiden, Jason A, Roose-Girma, Merone, Tam, Lucinda, Barck, Kai H, Carano, Richard A D, Ding, Han Ting, Brillantes, Bobby, Tam, Christine, Yang, Xiaoying, Gao, Simon S, Ly, Justin Q, Liu, Liling, Chen, Liuxi, Liederer, Bianca M, Lin, Joseph H, Magnuson, Steven, Chen, Jun, Hackos, David H, Elstrott, Justin, Rohou, Alexis, Safina, Brian S, Volgraf, Matthew, Bauer, Rebecca N, Riol-Blanco, Lorena
Published in The Journal of experimental medicine (05.04.2021)
Published in The Journal of experimental medicine (05.04.2021)
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Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain
Bankar, Girish, Goodchild, Samuel J., Howard, Sarah, Nelkenbrecher, Karen, Waldbrook, Matthew, Dourado, Michelle, Shuart, Noah G., Lin, Sophia, Young, Clint, Xie, Zhiwei, Khakh, Kuldip, Chang, Elaine, Sojo, Luis E., Lindgren, Andrea, Chowdhury, Sultan, Decker, Shannon, Grimwood, Michael, Andrez, Jean-Christophe, Dehnhardt, Christoph M., Pang, Jodie, Chang, Jae H., Safina, Brian S., Sutherlin, Daniel P., Johnson, James P., Hackos, David H., Robinette, C. Lee, Cohen, Charles J.
Published in Cell reports (Cambridge) (18.09.2018)
Published in Cell reports (Cambridge) (18.09.2018)
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Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors
Blake, James F, Xu, Rui, Bencsik, Josef R, Xiao, Dengming, Kallan, Nicholas C, Schlachter, Stephen, Mitchell, Ian S, Spencer, Keith L, Banka, Anna L, Wallace, Eli M, Gloor, Susan L, Martinson, Matthew, Woessner, Richard D, Vigers, Guy P.A, Brandhuber, Barbara J, Liang, Jun, Safina, Brian S, Li, Jun, Zhang, Birong, Chabot, Christine, Do, Steven, Lee, Leslie, Oeh, Jason, Sampath, Deepak, Lee, Brian B, Lin, Kui, Liederer, Bianca M, Skelton, Nicholas J
Published in Journal of medicinal chemistry (27.09.2012)
Published in Journal of medicinal chemistry (27.09.2012)
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Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy
Terrett, Jack A, Chen, Huifen, Shore, Daniel G, Villemure, Elisia, Larouche-Gauthier, Robin, Déry, Martin, Beaumier, Francis, Constantineau-Forget, Léa, Grand-Maître, Chantal, Lépissier, Luce, Ciblat, Stéphane, Sturino, Claudio, Chen, Yong, Hu, Baihua, Lu, Aijun, Wang, Yunli, Cridland, Andrew P, Ward, Stuart I, Hackos, David H, Reese, Rebecca M, Shields, Shannon D, Chen, Jun, Balestrini, Alessia, Riol-Blanco, Lorena, Lee, Wyne P, Liu, John, Suto, Eric, Wu, Xiumin, Zhang, Juan, Ly, Justin Q, La, Hank, Johnson, Kevin, Baumgardner, Matt, Chou, Kang-Jye, Rohou, Alexis, Rougé, Lionel, Safina, Brian S, Magnuson, Steven, Volgraf, Matthew
Published in Journal of medicinal chemistry (08.04.2021)
Published in Journal of medicinal chemistry (08.04.2021)
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Immune-stimulating antibody conjugates elicit robust myeloid activation and durable antitumor immunity
Ackerman, Shelley E, Pearson, Cecelia I, Gregorio, Joshua D, Gonzalez, Joseph C, Kenkel, Justin A, Hartmann, Felix J, Luo, Angela, Ho, Po Y, LeBlanc, Heidi, Blum, Lisa K, Kimmey, Samuel C, Luo, Andrew, Nguyen, Murray L, Paik, Jason C, Sheu, Lauren Y, Ackerman, Benjamin, Lee, Arthur, Li, Hai, Melrose, Jennifer, Laura, Richard P, Ramani, Vishnu C, Henning, Karla A, Jackson, David Y, Safina, Brian S, Yonehiro, Grant, Devens, Bruce H, Carmi, Yaron, Chapin, Steven J, Bendall, Sean C, Kowanetz, Marcin, Dornan, David, Engleman, Edgar G, Alonso, Michael N
Published in Nature cancer (01.01.2021)
Published in Nature cancer (01.01.2021)
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Discovery of TRPA1 Antagonist GDC-6599: Derisking Preclinical Toxicity and Aldehyde Oxidase Metabolism with a Potential First-in-Class Therapy for Respiratory Disease
Terrett, Jack A., Ly, Justin Q., Katavolos, Paula, Hasselgren, Catrin, Laing, Steven, Zhong, Fiona, Villemure, Elisia, Déry, Martin, Larouche-Gauthier, Robin, Chen, Huifen, Shore, Daniel G., Lee, Wyne P., Suto, Eric, Johnson, Kevin, Brooks, Marjory, Stablein, Alyssa, Beaumier, Francis, Constantineau-Forget, Léa, Grand-Maître, Chantal, Lépissier, Luce, Ciblat, Stéphane, Sturino, Claudio, Chen, Yong, Hu, Baihua, Elstrott, Justin, Gandham, Vineela, Joseph, Victory, Booler, Helen, Cain, Gary, Chou, Carolina, Fullerton, Aaron, Lepherd, Michelle, Stainton, Shannon, Torres, Elizabeth, Urban, Konnie, Yu, Lanlan, Zhong, Yu, Bao, Linda, Chou, Kang-Jye, Lin, Jessica, Zhang, Wei, La, Hank, Liu, Liling, Mulder, Teresa, Chen, Jun, Chernov-Rogan, Tania, Johnson, Adam R., Hackos, David H., Leahey, Rebecca, Shields, Shannon D., Balestrini, Alessia, Riol-Blanco, Lorena, Safina, Brian S., Volgraf, Matthew, Magnuson, Steven, Kakiuchi-Kiyota, Satoko
Published in Journal of medicinal chemistry (14.03.2024)
Published in Journal of medicinal chemistry (14.03.2024)
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Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain
McKerrall, Steven J, Nguyen, Teresa, Lai, Kwong Wah, Bergeron, Philippe, Deng, Lunbin, DiPasquale, Antonio, Chang, Jae H, Chen, Jun, Chernov-Rogan, Tania, Hackos, David H, Maher, Jonathan, Ortwine, Daniel F, Pang, Jodie, Payandeh, Jian, Proctor, William R, Shields, Shannon D, Vogt, Jennifer, Ji, Pengfei, Liu, Wenfeng, Ballini, Elisa, Schumann, Lilia, Tarozzo, Glauco, Bankar, Girish, Chowdhury, Sultan, Hasan, Abid, Johnson, J. P, Khakh, Kuldip, Lin, Sophia, Cohen, Charles J, Dehnhardt, Christoph M, Safina, Brian S, Sutherlin, Daniel P
Published in Journal of medicinal chemistry (25.04.2019)
Published in Journal of medicinal chemistry (25.04.2019)
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Identification of Selective Acyl Sulfonamide–Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity
Sun, Shaoyi, Jia, Qi, Zenova, Alla Y, Wilson, Michael S, Chowdhury, Sultan, Focken, Thilo, Li, Jun, Decker, Shannon, Grimwood, Michael E, Andrez, Jean-Christophe, Hemeon, Ivan, Sheng, Tao, Chen, Chien-An, White, Andy, Hackos, David H, Deng, Lunbin, Bankar, Girish, Khakh, Kuldip, Chang, Elaine, Kwan, Rainbow, Lin, Sophia, Nelkenbrecher, Karen, Sellers, Benjamin D, DiPasquale, Antonio G, Chang, Jae, Pang, Jodie, Sojo, Luis, Lindgren, Andrea, Waldbrook, Matthew, Xie, Zhiwei, Young, Clint, Johnson, James P, Robinette, C. Lee, Cohen, Charles J, Safina, Brian S, Sutherlin, Daniel P, Ortwine, Daniel F, Dehnhardt, Christoph M
Published in Journal of medicinal chemistry (24.01.2019)
Published in Journal of medicinal chemistry (24.01.2019)
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Discovery of a Potent (4R,5S)‑4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling
Chen, Huifen, Volgraf, Matthew, Do, Steven, Kolesnikov, Aleksandr, Shore, Daniel G, Verma, Vishal A, Villemure, Elisia, Wang, Lan, Chen, Yong, Hu, Baihua, Lu, Ai-Jun, Wu, Guosheng, Xu, Xiaofeng, Yuen, Po-wai, Zhang, Yamin, Erickson, Shawn D, Dahl, Martin, Brotherton-Pleiss, Christine, Tay, Suzanne, Ly, Justin Q, Murray, Lesley J, Chen, Jun, Amm, Desiree, Lange, Wienke, Hackos, David H, Reese, Rebecca M, Shields, Shannon D, Lyssikatos, Joseph P, Safina, Brian S, Estrada, Anthony A
Published in Journal of medicinal chemistry (26.04.2018)
Published in Journal of medicinal chemistry (26.04.2018)
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Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa V 1.7 Inhibitors for the Treatment of Pain
Focken, Thilo, Chowdhury, Sultan, Zenova, Alla, Grimwood, Michael E, Chabot, Christine, Sheng, Tao, Hemeon, Ivan, Decker, Shannon M, Wilson, Michael, Bichler, Paul, Jia, Qi, Sun, Shaoyi, Young, Clint, Lin, Sophia, Goodchild, Samuel J, Shuart, Noah G, Chang, Elaine, Xie, Zhiwei, Li, Bowen, Khakh, Kuldip, Bankar, Girish, Waldbrook, Matthew, Kwan, Rainbow, Nelkenbrecher, Karen, Karimi Tari, Parisa, Chahal, Navjot, Sojo, Luis, Robinette, C Lee, White, Andrew D, Chen, Chien-An, Zhang, Yi, Pang, Jodie, Chang, Jae H, Hackos, David H, Johnson, Jr, J P, Cohen, Charles J, Ortwine, Daniel F, Sutherlin, Daniel P, Dehnhardt, Christoph M, Safina, Brian S
Published in Journal of medicinal chemistry (14.06.2018)
Published in Journal of medicinal chemistry (14.06.2018)
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Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310
Safina, Brian S, McKerrall, Steven J, Sun, Shaoyi, Chen, Chien-An, Chowdhury, Sultan, Jia, Qi, Li, Jun, Zenova, Alla Y, Andrez, Jean-Christophe, Bankar, Girish, Bergeron, Philippe, Chang, Jae H, Chang, Elaine, Chen, Jun, Dean, Richard, Decker, Shannon M, DiPasquale, Antonio, Focken, Thilo, Hemeon, Ivan, Khakh, Kuldip, Kim, Amy, Kwan, Rainbow, Lindgren, Andrea, Lin, Sophia, Maher, Jonathan, Mezeyova, Janette, Misner, Dinah, Nelkenbrecher, Karen, Pang, Jodie, Reese, Rebecca, Shields, Shannon D, Sojo, Luis, Sheng, Tao, Verschoof, Henry, Waldbrook, Matthew, Wilson, Michael S, Xie, Zhiwei, Young, Clint, Zabka, Tanja S, Hackos, David H, Ortwine, Daniel F, White, Andrew D, Johnson, J.P, Robinette, C. Lee, Dehnhardt, Christoph M, Cohen, Charles J, Sutherlin, Daniel P
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
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Pyrrolobenzodiazepine Dimer Antibody–Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers
Gregson, Stephen J., Masterson, Luke A., Wei, Binqing, Pillow, Thomas H., Spencer, Susan D., Kang, Gyoung-Dong, Yu, Shang-Fan, Raab, Helga, Lau, Jeffrey, Li, Guangmin, Lewis Phillips, Gail D., Gunzner-Toste, Janet, Safina, Brian S., Ohri, Rachana, Darwish, Martine, Kozak, Katherine R., dela Cruz-Chuh, Josefa, Polson, Andrew, Flygare, John A., Howard, Philip W.
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
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Discovery of Acyl-sulfonamide Na v 1.7 Inhibitors GDC-0276 and GDC-0310
Safina, Brian S, McKerrall, Steven J, Sun, Shaoyi, Chen, Chien-An, Chowdhury, Sultan, Jia, Qi, Li, Jun, Zenova, Alla Y, Andrez, Jean-Christophe, Bankar, Girish, Bergeron, Philippe, Chang, Jae H, Chang, Elaine, Chen, Jun, Dean, Richard, Decker, Shannon M, DiPasquale, Antonio, Focken, Thilo, Hemeon, Ivan, Khakh, Kuldip, Kim, Amy, Kwan, Rainbow, Lindgren, Andrea, Lin, Sophia, Maher, Jonathan, Mezeyova, Janette, Misner, Dinah, Nelkenbrecher, Karen, Pang, Jodie, Reese, Rebecca, Shields, Shannon D, Sojo, Luis, Sheng, Tao, Verschoof, Henry, Waldbrook, Matthew, Wilson, Michael S, Xie, Zhiwei, Young, Clint, Zabka, Tanja S, Hackos, David H, Ortwine, Daniel F, White, Andrew D, Johnson, Jr, J P, Robinette, C Lee, Dehnhardt, Christoph M, Cohen, Charles J, Sutherlin, Daniel P
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
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Journal Article
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models
Focken, Thilo, Liu, Shifeng, Chahal, Navjot, Dauphinais, Maxim, Grimwood, Michael E, Chowdhury, Sultan, Hemeon, Ivan, Bichler, Paul, Bogucki, David, Waldbrook, Matthew, Bankar, Girish, Sojo, Luis E, Young, Clint, Lin, Sophia, Shuart, Noah, Kwan, Rainbow, Pang, Jodie, Chang, Jae H, Safina, Brian S, Sutherlin, Daniel P, Johnson, J. P, Dehnhardt, Christoph M, Mansour, Tarek S, Oballa, Renata M, Cohen, Charles J, Robinette, C. Lee
Published in ACS medicinal chemistry letters (10.03.2016)
Published in ACS medicinal chemistry letters (10.03.2016)
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Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist
Ahuja, Shivani, Mukund, Susmith, Deng, Lunbin, Khakh, Kuldip, Chang, Elaine, Ho, Hoangdung, Shriver, Stephanie, Young, Clint, Lin, Sophia, Johnson, J. P., Wu, Ping, Li, Jun, Coons, Mary, Tam, Christine, Brillantes, Bobby, Sampang, Honorio, Mortara, Kyle, Bowman, Krista K., Clark, Kevin R., Estevez, Alberto, Xie, Zhiwei, Verschoof, Henry, Grimwood, Michael, Dehnhardt, Christoph, Andrez, Jean–Christophe, Focken, Thilo, Sutherlin, Daniel P., Safina, Brian S., Starovasnik, Melissa A., Ortwine, Daniel F., Franke, Yvonne, Cohen, Charles J., Hackos, David H., Koth, Christopher M., Payandeh, Jian
Published in Science (American Association for the Advancement of Science) (18.12.2015)
Published in Science (American Association for the Advancement of Science) (18.12.2015)
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Discovery of Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition
Safina, Brian S, Baker, Stewart, Baumgardner, Matt, Blaney, Paul M, Chan, Bryan K, Chen, Yung-Hsiang, Cartwright, Matthew W, Castanedo, Georgette, Chabot, Christine, Cheguillaume, Arnaud J, Goldsmith, Paul, Goldstein, David M, Goyal, Bindu, Hancox, Timothy, Handa, Raj K, Iyer, Pravin S, Kaur, Jasmit, Kondru, Rama, Kenny, Jane R, Krintel, Sussie L, Li, Jun, Lesnick, John, Lucas, Matthew C, Lewis, Cristina, Mukadam, Sophie, Murray, Jeremy, Nadin, Alan J, Nonomiya, Jim, Padilla, Fernando, Palmer, Wylie S, Pang, Jodie, Pegg, Neil, Price, Steve, Reif, Karin, Salphati, Laurent, Savy, Pascal A, Seward, Eileen M, Shuttleworth, Stephen, Sohal, Sukhjit, Sweeney, Zachary K, Tay, Suzanne, Tivitmahaisoon, Parcharee, Waszkowycz, Bohdan, Wei, Binqing, Yue, Qin, Zhang, Chenghong, Sutherlin, Daniel P
Published in Journal of medicinal chemistry (28.06.2012)
Published in Journal of medicinal chemistry (28.06.2012)
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Journal Article
Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Na v 1.7 Inhibitors for the Treatment of Chronic Pain
McKerrall, Steven J, Nguyen, Teresa, Lai, Kwong Wah, Bergeron, Philippe, Deng, Lunbin, DiPasquale, Antonio, Chang, Jae H, Chen, Jun, Chernov-Rogan, Tania, Hackos, David H, Maher, Jonathan, Ortwine, Daniel F, Pang, Jodie, Payandeh, Jian, Proctor, William R, Shields, Shannon D, Vogt, Jennifer, Ji, Pengfei, Liu, Wenfeng, Ballini, Elisa, Schumann, Lilia, Tarozzo, Glauco, Bankar, Girish, Chowdhury, Sultan, Hasan, Abid, Johnson, Jr, J P, Khakh, Kuldip, Lin, Sophia, Cohen, Charles J, Dehnhardt, Christoph M, Safina, Brian S, Sutherlin, Daniel P
Published in Journal of medicinal chemistry (25.04.2019)
Published in Journal of medicinal chemistry (25.04.2019)
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Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles
Safina, Brian S, Elliott, Richard L, Forrest, Andrew K, Heald, Robert A, Murray, Jeremy M, Nonomiya, Jim, Pang, Jodie, Salphati, Laurent, Seward, Eileen M, Staben, Steven T, Ultsch, Mark, Wei, Binqing, Yang, Wenqian, Sutherlin, Daniel P
Published in ACS medicinal chemistry letters (14.09.2017)
Published in ACS medicinal chemistry letters (14.09.2017)
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Total Synthesis of Thiostrepton. Retrosynthetic Analysis and Construction of Key Building Blocks
Nicolaou, K. C, Safina, Brian S, Zak, Mark, Lee, Sang Hyup, Nevalainen, Marta, Bella, Marco, Estrada, Anthony A, Funke, Christian, Zécri, Frédéric J, Bulat, Stephan
Published in Journal of the American Chemical Society (10.08.2005)
Published in Journal of the American Chemical Society (10.08.2005)
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