T
Todd Groessl
Researcher at Genomics Institute of the Novartis Research Foundation
Publications - 12
Citations - 1503
Todd Groessl is an academic researcher from Genomics Institute of the Novartis Research Foundation. The author has contributed to research in topics: Farnesoid X receptor & Chagas disease. The author has an hindex of 11, co-authored 12 publications receiving 1206 citations.
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Journal ArticleDOI
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
Thomas H. Marsilje,Wei Pei,Bei Chen,Wenshuo Lu,Tetsuo Uno,Jin Yunho,Tao Jiang,Sungjoon Kim,Nanxin Li,Markus Warmuth,Yelena Sarkisova,Frank Sun,Auzon Steffy,AnneMarie Culazzo Pferdekamper,Allen G. Li,Sean B. Joseph,Young Kim,Bo Liu,Tove Tuntland,Xiaoming Cui,Nathanael S. Gray,Ruo Steensma,Yongqin Wan,Jiqing Jiang,Chopiuk Greg,Jie Li,W. Perry Gordon,Wendy Richmond,Kevin Johnson,Jonathan Chang,Todd Groessl,You-Qun He,Andrew Phimister,Alex Aycinena,Christian C. Lee,Badry Bursulaya,Donald S. Karanewsky,H. Martin Seidel,Jennifer L. Harris,Pierre-Yves Michellys +39 more
TL;DR: In this initial report, preliminary structure-activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684).
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Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery
Stephan Meister,David Plouffe,Kelli Kuhen,Ghislain M. C. Bonamy,Tao Wu,S. Whitney Barnes,Selina Bopp,Rachel Borboa,A. Taylor Bright,A. Taylor Bright,Jianwei Che,Steve Cohen,Neekesh V. Dharia,Kerstin Gagaring,Montip Gettayacamin,Perry Gordon,Todd Groessl,Nobutaka Kato,Marcus C. S. Lee,Case W. McNamara,David A. Fidock,Advait Nagle,Tae-gyu Nam,Wendy Richmond,Jason Roland,Matthias Rottmann,Matthias Rottmann,Bin Zhou,Patrick Froissard,Patrick Froissard,Richard Glynne,Dominique Mazier,Dominique Mazier,Jetsumon Sattabongkot,Peter G. Schultz,Tove Tuntland,John R. Walker,Yingyao Zhou,Arnab K. Chatterjee,Thierry T. Diagana,Elizabeth A. Winzeler,Elizabeth A. Winzeler +41 more
TL;DR: An imidazolopiperazine scaffold series was identified that was highly enriched among compounds active against Plasmodium liver stages and shows potent in vivo blood-stage therapeutic activity.
Journal ArticleDOI
Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness
Shilpi Khare,Advait Nagle,Agnes Biggart,Yin H. Lai,Fang Liang,Lauren C. Davis,S. Whitney Barnes,Casey J. N. Mathison,Elmarie Myburgh,Elmarie Myburgh,Mu-Yun Gao,J. Robert Gillespie,Xianzhong Liu,Jocelyn Tan,Monique Stinson,Ianne C. Rivera,Jaime Ballard,Vince Yeh,Todd Groessl,Glenn C. Federe,Hazel X. Y. Koh,John D. Venable,Badry Bursulaya,Michael Shapiro,Pranab Mishra,Glen Spraggon,Ansgar Brock,Jeremy C. Mottram,Jeremy C. Mottram,Frederick S. Buckner,Srinivasa P. S. Rao,Ben G. Wen,John R. Walker,Tove Tuntland,Valentina Molteni,Richard Glynne,Frantisek Supek +36 more
TL;DR: A selective inhibitor of the kinetoplastid proteasome (GNF6702) with unprecedented in vivo efficacy, which cleared parasites from mice in all three models of infection, underscores the possibility of developing a single class of drugs for these neglected diseases.
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Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH)
David C. Tully,David C. Tully,Paul Vincent Rucker,Chianelli Donatella,Jennifer A. Williams,Vidal Agnes,Phil B. Alper,Daniel Mutnick,Badry Bursulaya,James Schmeits,Xiangdong Wu,Dingjiu Bao,Jocelyn Zoll,Young Kim,Todd Groessl,Peter McNamara,H. Martin Seidel,Valentina Molteni,Bo Liu,Andrew Phimister,Sean B. Joseph,Bryan Laffitte +21 more
TL;DR: The discovery of 1 (tropifexor, LJN452), a novel and highly potent agonist of FXR is reported, which has advanced into phase 2 human clinical trials in patients with NASH and PBC.
Journal ArticleDOI
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
Gerald Lelais,Robert Epple,Thomas H. Marsilje,Yun O. Long,Matthew McNeill,Bei Chen,Wenshuo Lu,Jaganmohan Anumolu,Sangamesh Badiger,Badry Bursulaya,Michael DiDonato,Rina Fong,Jose Juarez,Jie Li,Mari Manuia,Daniel E. Mason,Perry Gordon,Todd Groessl,Kevin Johnson,Yong Jia,Shailaja Kasibhatla,Chun Li,John Isbell,Glen Spraggon,Bender Steven Lee,Pierre-Yves Michellys +25 more
TL;DR: The approach toward the discovery of 47 (EGF816, nazartinib), a novel, covalent mutant-selective EGFR inhibitor with equipotent activity on both oncogenic and T790M-resistant EGFR mutations, is described.