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SaveDiscovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT)
Koester, Dennis C.; Marx, Vanessa M.; Williams, Sarah; Jiricek, Jan; Dauphinais, Maxime; Rene, Olivier; Miller, Sarah L.; Zhang, Lei; Patra, Debjani; Chen, Yen-Liang; Cheung, Harry; Gable, Jonathan; Lakshminarayana, Suresh B.; Osborne, Colin; Galarneau, Jean-Rene; Kulkarni, Upendra; Richmond, Wendy; Bretz, Angela; Xiao, Linda; Supek, Frantisek; Wiesmann, Christian; Honnappa, Srinivas; Be, Celine; Maeser, Pascal; Kaiser, Marcel; Ritchie, Ryan; Barrett, Michael P.; Diagana, Thierry T.; Sarko, Christopher; Rao, Srinivasa P. S. Share Save Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of LeishmaniasesNagle, Advait; Biggart, Agnes; Be, Celine; Srinivas, Honnappa; Hein, Andreas; Caridha, Diana; Sciotti, Richard J.; Pybus, Brandon; Kreishman-Deitrick, Mara; Bursulaya, Badry; Lai, Yin H.; Gao, Mu-Yun; Liang, Fang; Mathison, Casey J. N.; Liu, Xiaodong; Yeh, Vince; Smith, Jeffrey; Lerario, Isabelle; Xie, Yongping; Chianelli, Donatella; Gibney, Michael; Berman, Ashley; Chen, Yen-Liang; Jiricek, Jan; Davis, Lauren C.; Liu, Xianzhong; Ballard, Jaime; Khare, Shilpi; Eggimann, Fabian Kurt; Luneau, Alexandre; Groessl, Todd; Shapiro, Michael; Richmond, Wendy; Johnson, Kevin; Rudewicz, Patrick J.; Rao, Srinivasa P. S.; Thompson, Christopher; Tuntland, Tove; Spraggon, Glen; Glynne, Richard J.; Supek, Frantisek; Wiesmann, Christian; Molteni, Valentina Share Save Stabilizing Inactive Conformations of MALT1 as an Effective Approach to Inhibit Its Protease ActivityHughes, Nicola; Erbel, Paul; Bornancin, Frederic; Wiesmann, Christian; Schiering, Nikolaus; Villard, Frederic; Decock, Arnaud; Rubi, Bertran; Melkko, Samu; Spanka, Carsten; Buschmann, Nicole; Pissot-Soldermann, Carole; Simic, Oliver; Beerli, Rene; Sorge, Mickael; Tintelnot-Blomley, Marina; Beltz, Karen; Regnier, Catherine H.; Quancard, Jean; Schlapbach, Achim; Langlois, Jean-Baptiste; Renatus, Martin Share Save Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated DiseasesMainolfi, Nello; Ehara, Takeru; Karki, Rajeshri G.; Anderson, Karen; Mac Sweeney, Aengus; Liao, Sha-Mei; Argikar, Upendra A.; Jendza, Keith; Zhang, Chun; Powers, James; Klosowski, Daniel W.; Crowley, Maura; Kawanami, Toshio; Ding, Jian; April, Myriam; Forster, Cornelia; Serrano-Wu, Michael; Capparelli, Michael; Ramqaj, Rrezarta; Solovay, Catherine; Cumin, Frederic; Smith, Thomas M.; Ferrara, Luciana; Lee, Wendy; Long, Debby; Prentiss, Melissa; De Erkenez, Andrea; Yang, Louis; Liu, Fang; Sellner, Holger; Sirockin, Finton; Valeur, Eric; Erbel, Paulus; Ostermeier, Daniela; Ramage, Paul; Gerhartz, Bernd; Schubart, Anna; Flohr, Stefanie; Gradoux, Nathalie; Feifel, Roland; Vogg, Barbara; Wiesmann, Christian; Maibaum, Juergen; Eder, Joerg; Sedrani, Richard; Harrison, Richard A.; Mogi, Muneto; Jaffee, Bruce D.; Adams, Christopher M. Share Save Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin InhibitorsKawanami, Toshio; Karki, Rajeshri G.; Cody, Emma; Liu, Qian; Liang, Guiqing; Ksander, Gary M.; Rigel, Dean F.; Schiering, Nikolaus; Gong, Yongjin; Coppola, Gary M.; Iwaki, Yuki; Sun, Robert; Neubert, Alan; Fan, Li; Ingles, Sara; D'Arcy, Allan; Villard, Frederic; Ramage, Paul; Jeng, Arco Y.; Leung-Chu, Jennifer; Liu, Jing; Beil, Michael; Fu, Fumin; Chen, Wei; Cumin, Frederic; Wiesmann, Christian; Mogi, Muneto Share Save Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex (vol 85, pg 231, 2019)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 Share Save Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complexBussiere, 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 Share Save A small-molecule inhibitor of C5 complement proteinJendza, Keith; Kato, Mitsunori; Salcius, Michael; Srinivas, Honnappa; De Erkenez, Andrea; Nguyen, Anh; McLaughlin, Doug; Be, Celine; Wiesmann, Christian; Murphy, Jason; Bolduc, Philippe; Mogi, Muneto; Duca, Jose; Namil, Abdel; Capparelli, Michael; Darsigny, Veronique; Meredith, Erik; Tichkule, Ritesh; Ferrara, Luciana; Heyder, Jessica; Liu, Fang; Horton, Patricia A.; Romanowski, Michael J.; Schirle, Markus; Mainolfi, Nello; Anderson, Karen; Michaud, Gregory A. Share Save Small-molecule factor B inhibitor for the treatment of complement-mediated diseasesSchubart, Anna; Anderson, Karen; Mainolfi, Nello; Sellner, Holger; Ehara, Takeru; Adams, Christopher M.; Mac Sweeney, Aengus; Liao, Sha-Mei; Crowley, Maura; Littlewood-Evans, Amanda; Sarret, Sophie; Wieczorek, Grazyna; Perrot, Ludovic; Dubost, Valerie; Flandre, Thierry; Zhang, Yuzhou; Smith, Richard J. H.; Risitano, Antonio M.; Karki, Rajeshri G.; Zhang, Chun; Valeur, Eric; Sirockin, Finton; Gerhartz, Bernd; Erbel, Paulus; Hughes, Nicola; Smith, Thomas M.; Cumin, Frederic; Argikar, Upendra A.; Haraldsson, Boerje; Mogi, Muneto; Sedrani, Richard; Wiesmann, Christian; Jaffee, Bruce; Maibaum, Juergen; Flohr, Stefanie; Harrison, Richard; Eder, Joerg Share Save Human Memory B Cells Harbor Diverse Cross-Neutralizing Antibodies against BK and JC PolyomavirusesLindner, John M.; Cornacchione, Vanessa; Sathe, Atul; Be, Celine; Srinivas, Honnappa; Riquet, Elodie; Leber, Xavier-Charles; Hein, Andreas; Wrobel, Matthias B.; Scharenberg, Meike; Pietzonka, Thomas; Wiesmann, Christian; Abend, Johanna; Traggiai, Elisabetta Share Save Share Save Targeted inhibition of the COP9 signalosome for treatment of cancerSchlierf, Anita; Altmann, Eva; Quancard, Jean; Jefferson, Anne B.; Assenberg, Rene; Renatus, Martin; Jones, Matthew; Hassiepen, Ulrich; Schaefer, Michael; Kiffe, Michael; Weiss, Andreas; Wiesmann, Christian; Sedrani, Richard; Eder, Jorg; Martoglio, Bruno Share Save Structure of neprilysin in complex with the active metabolite of sacubitrilSchiering, Nikolaus; D'Arcy, Allan; Villard, Frederic; Ramage, Paul; Logel, Claude; Cumin, Frederic; Ksander, Gary M.; Wiesmann, Christian; Karki, Rajeshri G.; Mogi, Muneto Share Save Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1Gazzard, Lewis; Williams, Karen; Chen, Huifen; Axford, Lorraine; Blackwood, Elizabeth; Burton, Brenda; Chapman, Kerry; Crackett, Peter; Drobnick, Joy; Ellwood, Charles; Epler, Jennifer; Flagella, Michael; Gancia, Emanuela; Gill, Matthew; Goodacre, Simon; Halladay, Jason; Hewitt, Joanne; Hunt, Hazel; Kintz, Samuel; Lyssikatos, Joseph; Macleod, Calum; Major, Sarah; Medard, Guillaume; Narukulla, Raman; Ramiscal, Judi; Schmidt, Stephen; Seward, Eileen; Wiesmann, Christian; Wu, Ping; Yee, Sharon; Yen, Ivana; Malek, Shiva Share Save Share Save Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors.Olivero, Alan G.; Heffron, Timothy P.; Baumgardner, Matthew; Belvin, Marcia; Ross, Leanne Berry; Blaquiere, Nicole; Bradley, Erin; Castanedo, Georgette; Derynck, Mika; Do, Steven; Dotson, Jennafer; Dudley, Danette; Edgar, Kyle; Folkes, Adrian; Francis, Ross; Gianetti, Tony; Goldsmith, Richard; Goldsmith, Paul; Guan, Jane; Harrison, Trevor; Heald, Robert; Hsu, Jerry; Jackson, Phillip; Jones, Graham; Kim, Amy; Kolesnikov, Aleks; Lackner, Mark; Lee, Leslie; Lesnick, John; Lewis, Cristina; Mamounas, Michael; McLean, Neville; Murray, Jeremy; Ndubaku, Chudi; Nonomiya, Jim; Pang, Jodie; Pegg, Neil; Prior, Wei Wei; Salphati, Laurent; Sampath, Deepack; Sideris, Stephen; Siu, Michael; Staben, Steven; Sutherlin, Daniel; Ultsch, Mark; Wallin, Jeff; Wang, Lan; Wiesmann, Christian; Zhang, Xiaolin; Friedman, Lori S. Share Save Discovery of Novel Allosteric Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors Possessing Bidentate Ser212 InteractionsHeald, Robert A.; Jackson, Philip; Savy, Pascal; Jones, Mark; Gancia, Emanuela; Burton, Brenda; Newman, Richard; Boggs, Jason; Chan, Emily; Chan, Jocelyn; Choo, Edna; Merchant, Mark; Rudewicz, Patrick; Ultsch, Mark; Wiesmann, Christian; Yue, Qin; Belvin, Marcia; Price, Steve Share Save Inhibiting Alternative Pathway Complement Activation by Targeting the Factor D ExositeKatschke, Kenneth J., Jr.; Wu, Ping; Ganesan, Rajkumar; Kelley, Robert F.; Mathieu, Mary A.; Hass, Philip E.; Murray, Jeremy; Kirchhofer, Daniel; Wiesmann, Christian; Campagne, Menno van Lookeren Share Save Structure of TIGIT immunoreceptor bound to poliovirus receptor reveals a cell-cell adhesion and signaling mechanism that requires cis-trans receptor clusteringStengel, Katharina F.; Harden-Bowles, Kristin; Yu, Xin; Rouge, Lionel; Yin, Jianping; Comps-Agrar, Laetitia; Wiesmann, Christian; Bazan, J. Fernando; Eaton, Dan L.; Grogan, Jane L. Share Save 
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