Potent Inhibitors of Plasmodial Serine Hydroxymethyltransferase (SHMT) Featuring a Spirocyclic Scaffold

by Geoffrey Schwertz, Matthias C. Witschel, Matthias Rottmann, Ubolsree Leartsakulpanich, Penchit Chitnumsub, Aritsara Jaruwat, Watcharee Amornwatcharapong, Wanwipa Ittarat, Anja Schäfer, Raphael A. Aponte, Nils Trapp, Pimchai Chaiyen, François Diederich
Published 2019

Conformational Aspects in the Design of Inhibitors for Serine Hydroxymethyltransferase (SHMT): Biphenyl, Aryl Sulfonamide, and Aryl Sulfone Motifs

by Geoffrey Schwertz, Michelle S. Frei, Matthias C. Witschel, Matthias Rottmann, Ubolsree Leartsakulpanich, Penchit Chitnumsub, Aritsara Jaruwat, Wanwipa Ittarat, Anja Schäfer, Raphael A. Aponte, Nils Trapp, Kerstin Mark, Pimchai Chaiyen, François Diederich
Published 2018

Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures

by Geoffrey Schwertz, Matthias C. Witschel, Matthias Rottmann, Roger Bonnert, Ubolsree Leartsakulpanich, Penchit Chitnumsub, Aritsara Jaruwat, Wanwipa Ittarat, Anja Schäfer, Raphael A. Aponte, Susan A. Charman, Karen L. White, Abhijit Kundu, Surajit Sadhukhan, Mel Lloyd, Gail M. Freiberg, Myron Srikumaran, Marc Siggel, Adrian Zwyssig, Pimchai Chaiyen, François Diederich
Published 2018

Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): Cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities

by Matthias C. Witschel, Matthias Rottmann, Anatol Schwab, Ubolsree Leartsakulpanich, Penchit Chitnumsub, Michael Seet, Sandro Tonazzi, Geoffrey Schwertz, Frank Stelzer, Thomas Mietzner, Case McNamara, Frank Thater, Céline Freymond, Aritsara Jaruwat, Chatchadaporn Pinthong, Pinpunya Riangrungroj, Mouhssin Oufir, Matthias Hamburger, Pascal Mäser, Laura M. Sanz-Alonso, Susan Charman, Sergio Wittlin, Yongyuth Yuthavong, Pimchai Chaiyen, François Diederich
Published 2018

Spiroindolones, a potent compound class for the treatment of malaria

by Matthias Rottmann, Case McNamara, Bryan K.S. Yeung, Marcus C.S. Lee, Bin Zou, Bruce Russell, Patrick Seitz, David M. Plouffe, Neekesh V. Dharia, Jocelyn Tan, Steven B. Cohen, Kathryn R. Spencer, Gonzalo E. González-Páez, Suresh B. Lakshminarayana, Anne Goh, Rossarin Suwanarusk, Timothy Jegla, Esther K. Schmitt, Hans Peter Beck, Reto Brun, Francois Nosten, Laurent Renia, Veronique Dartois, Thomas H. Keller, David A. Fidock, Elizabeth A. Winzeler, Thierry T. Diagana
Published 2018

KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission

by Kelli L. Kuhen, Arnab K. Chatterjee, Matthias Rottmann, Kerstin Gagaring, Rachel Borboa, Jennifer Buenviaje, Zhong Chen, Carolyn Francek, Tao Wu, Advait Nagle, S. Whitney Barnes, David Plouffe, Marcus C.S. Lee, David A. Fidock, Wouter Graumans, Marga Van De Vegte-Bolmer, Geert J. Van Gemert, Grennady Wirjanata, Boni Sebayang, Jutta Marfurt, Bruce Russell, Rossarin Suwanarusk, Ric N. Price, Francois Nosten, Anchalee Tungtaeng, Montip Gettayacamin, Jetsumon Sattabongkot, Jennifer Taylor, John R. Walker, David Tully, Kailash P. Patra, Erika L. Flannery, Joseph M. Vinetz, Laurent Renia, Robert W. Sauerwein, Elizabeth A. Winzeler, Richard J. Glynne, Thierry T. Diagana
Published 2018

Targeting Plasmodium PI(4)K to eliminate malaria

by Case W. McNamara, Marcus C.S. Lee, Chek Shik Lim, Siau Hoi Lim, Jason Roland, Advait Nagle, Oliver Simon, Bryan K.S. Yeung, Arnab K. Chatterjee, Susan L. McCormack, Micah J. Manary, Anne Marie Zeeman, Koen J. Dechering, T. R.Santha Kumar, Philipp P. Henrich, Kerstin Gagaring, Maureen Ibanez, Nobutaka Kato, Kelli L. Kuhen, Christoph Fischli, Matthias Rottmann, David M. Plouffe, Badry Bursulaya, Stephan Meister, Lucia Rameh, Joerg Trappe, Dorothea Haasen, Martijn Timmerman, Robert W. Sauerwein, Rossarin Suwanarusk, Bruce Russell, Laurent Renia, Francois Nosten, David C. Tully, Clemens H.M. Kocken, Richard J. Glynne, Christophe Bodenreider, David A. Fidock, Thierry T. Diagana, Elizabeth A. Winzeler
Published 2018