Search Results - "Groessl, Todd"

Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH) by Tully, David C, Rucker, Paul V, Chianelli, Donatella, Williams, Jennifer, Vidal, Agnès, Alper, Phil B, Mutnick, Daniel, Bursulaya, Badry, Schmeits, James, Wu, Xiangdong, Bao, Dingjiu, Zoll, Jocelyn, Kim, Young, Groessl, Todd, McNamara, Peter, Seidel, H. Martin, Molteni, Valentina, Liu, Bo, Phimister, Andrew, Joseph, Sean B, Laffitte, Bryan

“…The farnesoid X receptor (FXR) is a nuclear receptor that acts as a master regulator of bile acid metabolism and signaling. Activation of FXR inhibits bile…”
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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5‑Chloro‑N2‑(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)‑N4‑(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials by 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

“…The synthesis, preclinical profile, and in vivo efficacy in rat xenograft models of the novel and selective anaplastic lymphoma kinase inhibitor 15b (LDK378)…”
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Integrating pharmacokinetic-pharmacodynamic modeling in preclinical assessment of mutant selective EGFR covalent tyrosine kinase inhibitor EGF816 by 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

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A Chemically Induced Vaccine Strategy for Prostate Cancer by Dubrovska, Anna, Kim, Chanhyuk, Elliott, Jimmy, Shen, Weijun, Kuo, Tun-Hsun, Koo, Dong-In, Li, Chun, Tuntland, Tove, Chang, Jonathan, Groessl, Todd, Wu, Xu, Gorney, Vanessa, Ramirez-Montagut, Teresa, Spiegel, David A, Cho, Charles Y, Schultz, Peter G

“…Here we report the design and evaluation of a bifunctional, small molecule switch that induces a targeted immune response against tumors in vivo. A high…”
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Characterization of IDN-6556 (3-[2-(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]-4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid): a liver-targeted caspase inhibitor by Hoglen, Niel C, Chen, Long-Shiuh, Fisher, Craig D, Hirakawa, Brad P, Groessl, Todd, Contreras, Patricia C

“…The potency, efficacy, and pharmacokinetic properties of IDN-6556…”
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Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness by Khare, Shilpi, Nagle, Advait S., Biggart, Agnes, Lai, Yin H., Liang, Fang, Davis, Lauren C., Barnes, S. Whitney, Mathison, Casey J. N., Myburgh, Elmarie, Gao, Mu-Yun, Gillespie, J. Robert, Liu, Xianzhong, Tan, Jocelyn L., Stinson, Monique, Rivera, Ianne C., Ballard, Jaime, Yeh, Vince, Groessl, Todd, Federe, Glenn, Koh, Hazel X. Y., Venable, John D., Bursulaya, Badry, Shapiro, Michael, Mishra, Pranab K., Spraggon, Glen, Brock, Ansgar, Mottram, Jeremy C., Buckner, Frederick S., Rao, Srinivasa P. S., Wen, Ben G., Walker, John R., Tuntland, Tove, Molteni, Valentina, Glynne, Richard J., Supek, Frantisek

“…A selective inhibitor of the kinetoplastid proteasome (GNF6702) is identified that is highly efficacious in vivo , clearing the parasites that cause…”
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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 by 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

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Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis by Chianelli, Donatella, Rucker, Paul V, Roland, Jason, Tully, David C, Nelson, John, Liu, Xiaodong, Bursulaya, Badry, Hernandez, Eloy D, Wu, Jane, Prashad, Mahavir, Schlama, Thierry, Liu, Yugang, Chu, Alan, Schmeits, James, Huang, David J, Hill, Robert, Bao, Dingjiu, Zoll, Jocelyn, Kim, Young, Groessl, Todd, McNamara, Peter, Liu, Bo, Richmond, Wendy, Sancho-Martinez, Ignacio, Phimister, Andrew, Seidel, H. Martin, Badman, Michael K, Joseph, Sean B, Laffitte, Bryan, Molteni, Valentina

“…Farnesoid X receptor (FXR) agonists are emerging as important potential therapeutics for the treatment of nonalcoholic steatohepatitis (NASH) patients, as they…”
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Antitrypanosomal Treatment with Benznidazole Is Superior to Posaconazole Regimens in Mouse Models of Chagas Disease by Khare, Shilpi, Liu, Xianzhong, Stinson, Monique, Rivera, Ianne, Groessl, Todd, Tuntland, Tove, Yeh, Vince, Wen, Ben, Molteni, Valentina, Glynne, Richard, Supek, Frantisek

“…Two CYP51 inhibitors, posaconazole and the ravuconazole prodrug E1224, were recently tested in clinical trials for efficacy in indeterminate Chagas disease…”
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Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases by Nagle, 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

“…Visceral leishmaniasis is responsible for up to 30,000 deaths every year. Current treatments have shortcomings that include toxicity and variable efficacy…”
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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 by 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

“…Over the past decade, first and second generation EGFR inhibitors have significantly improved outcomes for lung cancer patients with activating mutations in…”
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Use of solubilizers in preclinical formulations: Effect of Cremophor EL on the pharmacokinetic properties on early discovery compounds by Liu, Bo, Gordon, William Perry, Richmond, Wendy, Groessl, Todd, Tuntland, Tove

“…The aim of the present study was to determine whether Cremophor EL is a suitable surfactant that can be routinely applied to pharmacokinetic (PK) studies in…”
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Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery by Meister, Stephan, Plouffe, David M., Kuhen, Kelli L., Bonamy, Ghislain M. C., Wu, Tao, Barnes, S. Whitney, Bopp, Selina E., Borboa, Rachel, Bright, A. Taylor, Che, Jianwei, Cohen, Steve, Dharia, Neekesh V., Gagaring, Kerstin, Gettayacamin, Montip, Gordon, Perry, Groessl, Todd, Kato, Nobutaka, Lee, Marcus C. S., McNamara, Case W., Fidock, David A., Nagle, Advait, Nam, Tae-gyu, Richmond, Wendy, Roland, Jason, Rottmann, Matthias, Zhou, Bin, Froissard, Patrick, Glynne, Richard J., Mazier, Dominique, Sattabongkot, Jetsumon, Schultz, Peter G., Tuntland, Tove, Walker, John R., Zhou, Yingyao, Chatterjee, Arnab, Diagana, Thierry T., Winzeler, Elizabeth A.

“…Most malaria drug development focuses on parasite stages detected in red blood cells, even though, to achieve eradication, next-generation drugs active against…”
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A modern in vivo pharmacokinetic paradigm: combining snapshot, rapid and full PK approaches to optimize and expedite early drug discovery by Li, Chun, Liu, Bo, Chang, Jonathan, Groessl, Todd, Zimmerman, Matthew, He, You-Qun, Isbell, John, Tuntland, Tove

“…► Three tiered in vivo rodent PK approaches (snapshot, rapid and full PK studies) at GNF are described. ► Applications and utilities of each in vivo PK…”
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Discovery of ( R , E )- N -(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1 H -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 by 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

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Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists by 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

“…[Display omitted] Systematic SAR optimization of the GPR119 agonist lead 1, derived from an internal HTS campaign, led to compound 29. Compound 29 displays…”
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First-in-Class Pan Caspase Inhibitor Developed for the Treatment of Liver Disease by Linton, Steven D, Aja, Teresa, Armstrong, Robert A, Bai, Xu, Chen, Long-Shiuh, Chen, Ning, Ching, Brett, Contreras, Patricia, Diaz, Jose-Luis, Fisher, Craig D, Fritz, Lawrence C, Gladstone, Patricia, Groessl, Todd, Gu, Xin, Herrmann, Julia, Hirakawa, Brad P, Hoglen, Niel C, Jahangiri, Kathy G, Kalish, Vincent J, Karanewsky, Donald S, Kodandapani, Lalitha, Krebs, Joseph, McQuiston, Jeff, Meduna, Steven P, Nalley, Kip, Robinson, Edward D, Sayers, Robert O, Sebring, Kristen, Spada, Alfred P, Ternansky, Robert J, Tomaselli, Kevin J, Ullman, Brett R, Valentino, Karen L, Weeks, Suzanne, Winn, David, Wu, Joe C, Yeo, Pauline, Zhang, Cheng-zhi

“…A series of oxamyl dipeptides were optimized for pan caspase inhibition, anti-apoptotic cellular activity and in vivo efficacy. This structure−activity…”
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