Publications

Walz A, Sax S, Scheurer C, Tamasi B, Mäser P, Wittlin S. Incomplete Plasmodium falciparum growth inhibition following piperaquine treatment translates into increased parasite viability in the in vitro parasite reduction ratio assay. Front Cell Infect Microbiol. 2024;14:1396786. DOI: 10.3389/fcimb.2024.1396786

Ling D.B, Nguyen W, Looker O, Razook Z, McCann K, Barry A.E, Scheurer C, Wittlin S, Famodimu M.T, Delves M.J, Bullen H.E, Crabb B.S, Sleebs B.E, Gilson P.R. A pyridyl-furan series developed from the Open Global Health Library block red blood cell invasion and protein trafficking in Plasmodium falciparum through potential inhibition of the parasite's PI4KIIIB enzyme. ACS Infect Dis. 2023;9(9):1695-1710. DOI: 10.1021/acsinfecdis.3c00138

Ren R, Wang X, Leas D.A, Scheurer C, Hövel S, Cal M, Chen G, Zhong L, Katneni K, Pham T, Patil R, Sil D, Walters M.J, Schulze T.T, Neville A.J, Dong Y, Wittlin S, Kaiser M, Davis P.H, Charman S.A, Vennerstrom J.L. Antimalarial dibenzannulated medium-ring keto lactams. ACS Infect Dis. 2023;9(10):1964-1980. DOI: 10.1021/acsinfecdis.3c00245

Hitz E, Grüninger O, Passecker A, Wyss M, Scheurer C, Wittlin S, Beck H.P, Brancucci N.M.B, Voss T.S. The catalytic subunit of Plasmodium falciparum casein kinase 2 is essential for gametocytogenesis. Commun Biol. 2021;4(1):336. DOI: 10.1038/s42003-021-01873-0

Hitz E, Wiedemar N, Passecker A, Graça B.A.S, Scheurer C, Wittlin S, Brancucci N.M.B, Vakonakis I, Mäser P, Voss T.S. The 3-phosphoinositide-dependent protein kinase 1 is an essential upstream activator of protein kinase A in malaria parasites. PLoS Biol. 2021;19(12):e3001483. DOI: 10.1371/journal.pbio.3001483

Shackleford D.M, Chiu F.C.K, Katneni K, Blundell S, McLaren J, Wang X, Zhou L, Sriraghavan K, Alker A.M, Hunziker D, Scheurer C, Zhao Q, Dong Y, Mohrle J.J, Abla N, Matile H, Wittlin S, Vennerstrom J.L, Charman S.A. Cytochrome P450-mediated metabolism and CYP Inhibition for the synthetic peroxide antimalarial OZ439. ACS Infect Dis. 2021;7(7):1885-1893. DOI: 10.1021/acsinfecdis.1c00225

Schalkwijk J, Allman E.L, Jansen P.A.M, de Vries L.E, Verhoef J.M.J, Jackowski S, Botman P.N.M, Beuckens-Schortinghuis C.A, Koolen K.M.J, Bolscher J.M, Vos M.W, Miller K, Reeves S.A, Pett H, Trevitt G, Wittlin S, Scheurer C, Sax S, Fischli C, Angulo-Barturen I, Jimenez-Diaz M.B, Josling G, Kooij T.W.A, Bonnert R, Campo B, Blaauw R.H, Rutjes Fpjt, Sauerwein R.W, Llinas M, Hermkens P.H.H, Dechering K.J. Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in Plasmodium falciparum. Sci Transl Med. 2019;11(510):eaas9917. DOI: 10.1126/scitranslmed.aas9917

Baumgärtner F, Jourdan J, Scheurer C, Blasco B, Campo B, Mäser P, Wittlin S. In vitro activity of anti-malarial ozonides against an artemisinin-resistant isolate. Malar J. 2017;16:45. DOI: 10.1186/s12936-017-1696-0

Dong Y, Wang X, Kamaraj S, Bulbule V.J, Chiu F.C, Chollet J, Dhanasekaran M, Hein C.D, Papastogiannidis P, Morizzi J, Shackleford D.M, Barker H, Ryan E, Scheurer C, Tang Y, Zhao Q, Zhou L, White K.L, Urwyler H, Charman W.N, Matile H, Wittlin S, Charman S.A, Vennerstrom J.L. Structure-activity relationship of the antimalarial ozonide artefenomel (OZ439). J Med Chem. 2017;60(7):2654-2668. DOI: 10.1021/acs.jmedchem.6b01586

Paquet T, Le Manach C, Cabrera D.G, Younis Y, Henrich P.P, Abraham T.S, Lee M.C.S, Basak R, Ghidelli-Disse S, Lafuente-Monasterio M.J, Bantscheff M, Ruecker A, Blagborough A.M, Zakutansky S.E, Zeeman A.M, White K.L, Shackleford D.M, Mannila J, Morizzi J, Scheurer C, Angulo-Barturen I, Martinez M.S, Ferrer S, Sanz L.M, Gamo F.J, Reader J, Botha M, Dechering K.J, Sauerwein R.W, Tungtaeng A, Vanachayangkul P, Lim C.S, Burrows J, Witty M.J, Marsh K.C, Bodenreider C, Rochford R, Solapure S.M, Jimenez-Diaz M.B, Wittlin S, Charman S.A, Donini C, Campo B, Birkholtz L.M, Hanson K.K, Drewes G, Kocken C.H.M, Delves M.J, Leroy D, Fidock D.A, Waterson D, Street L.J, Chibale K. Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase. Sci Transl Med. 2017;9(387):eaad9735. DOI: 10.1126/scitranslmed.aad9735

Le Bihan A, de Kanter R, Angulo-Barturen I, Binkert C, Boss C, Brun R, Brunner R, Buchmann S, Burrows J, Dechering K.J, Delves M, Ewerling S, Ferrer S, Fischli C, Gamo-Benito F.J, Gnadig N.F, Heidmann B, Jimenez-Diaz M.B, Leroy D, Martinez M.S, Meyer S, Moehrle J.J, Ng C.L, Noviyanti R, Ruecker A, Sanz L.M, Sauerwein R.W, Scheurer C, Schleiferboeck S, Sinden R, Snyder C, Straimer J, Wirjanata G, Marfurt J, Price R.N, Weller T, Fischli W, Fidock D.A, Clozel M, Wittlin S. Characterization of novel antimalarial compound ACT-451840: preclinical assessment of activity and dose-efficacy modeling. PLoS Med. 2016;13(10):e1002138. DOI: 10.1371/journal.pmed.1002138

Chugh M, Scheurer C, Sax S, Bilsland E, van Schalkwyk D.A, Wicht K.J, Hofmann N, Sharma A, Bashyam S, Singh S, Oliver S.G, Egan T.J, Malhotra P, Sutherland C.J, Beck H.P, Wittlin S, Spangenberg T, Ding X.C. Identification and deconvolution of cross-resistance signals from antimalarial compounds using multidrug-resistant Plasmodium falciparum strains. Antimicrob Agents Chemother. 2015;59(2):1110-1118. DOI: 10.1128/AAC.03265-14

Mizukawa Y, Ge J.F, Bakar Md A, Itoh I, Scheurer C, Wittlin S, Brun R, Matsuoka H, Ihara M. Novel synthetic route for antimalarial benzo[a]phenoxazine derivative SSJ-183 and two active metabolites. Bioorg Med Chem. 2014;22(14):3749-3752. DOI: 10.1016/j.bmc.2014.04.066

Le Manach C, Scheurer C, Sax S, Schleiferböck S, Gonzalez Cabrera D, Younis Y, Paquet T, Street L, Smith P, Ding X, Waterson D, Witty M.J, Leroy D, Chibale K, Wittlin S. Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum. Malar J. 2013;12:424. DOI: 10.1186/1475-2875-12-424

Schleiferböck S, Scheurer C, Ihara M, Itoh I, Bathurst I, Burrows J.N, Fantauzzi P, Lotharius J, Charman S.A, Morizzi J, Shackleford D.M, White K.L, Brun R, Wittlin S. In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models. Drug Des Devel Ther. 2013;7:1377-1384. DOI: 10.2147/DDDT.S51298

Wang X, Dong Y, Wittlin S, Charman S.A, Chiu F.C, Chollet J, Katneni K, Mannila J, Morizzi J, Ryan E, Scheurer C, Steuten J, Santo Tomas J, Snyder C, Vennerstrom J.L. Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres. J Med Chem. 2013;56(6):2547-2555. DOI: 10.1021/jm400004u

Delves M, Plouffe D, Scheurer C, Meister S, Wittlin S, Winzeler E.A, Sinden R.E, Leroy D. The activities of current antimalarial drugs on the life cycle stages of Plasmodium: a comparative study with human and rodent parasites. PLoS Med. 2012;9(2):e1001169. DOI: 10.1371/journal.pmed.1001169

González Cabrera D, Douelle F, Younis Y.E, Feng T.S, Lemanach C, Nchinda A.T, Street L.J, Scheurer C, Kamber J, White K.L, Montagnat O.D, Ryan E, Katneni K, Zabiulla K.M, Joseph J.T, Bashyam S, Waterson D, Witty M.J, Charman S.A, Wittlin S, Chibale K. Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines. J Med Chem. 2012;55(24):11022-11030. DOI: 10.1021/jm301476b

Wenzler T, Steinhuber A, Wittlin S, Scheurer C, Brun R, Trampuz A. Isothermal microcalorimetry, a new tool to monitor drug action against Trypanosoma brucei and Plasmodium falciparum. PLoS Negl Trop Dis. 2012;6(6):e1668. DOI: 10.1371/journal.pntd.0001668

Charman S.A, Arbe-Barnes S, Bathurst I.C, Brun R, Campbell M, Charman W.N, Chiu F.C, Chollet J, Craft J.C, Creek D.J, Dong Y, Matile H, Maurer M, Morizzi J, Nguyen T, Papastogiannidis P, Scheurer C, Shackleford D.M, Sriraghavan K, Stingelin L, Tang Y, Urwyler H, Wang X, White K.L, Wittlin S, Zhou L, Vennerstrom J.L. Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria. Proc Natl Acad Sci USA. 2011;108(11):4400-4405. DOI: 10.1073/pnas.1015762108

Dong Y, Wittlin S, Sriraghavan K, Chollet J, Charman S.A, Charman W.N, Scheurer C, Urwyler H, Santo Tomas J, Snyder C, Creek D.J, Morizzi J, Koltun M, Matile H, Wang X, Padmanilayam M, Tang Y, Dorn A, Brun R, Vennerstrom J.L. The structure-activity relationship of the antimalarial ozonide arterolane (OZ277). J Med Chem. 2010;53(1):481-491. DOI: 10.1021/jm901473s

Geist J.G, Lauw S, Illarionova V, Illarionov B, Fischer M, Grawert T, Rohdich F, Eisenreich W, Kaiser J, Groll M, Scheurer C, Wittlin S, Alonso-Gomez J.L, Schweizer W.B, Bacher A, Diederich F. Thiazolopyrimidine inhibitors of 2-methylerythritol 2,4-cyclodiphosphate synthase (IspF) from Mycobacterium tuberculosis and Plasmodium falciparum. ChemMedChem. 2010;5(7):1092-1101. DOI: 10.1002/cmdc.201000083

Tang Y, Wittlin S, Charman S.A, Chollet J, Chiu F.C, Morizzi J, Johnson L.M, Tomas J.S, Scheurer C, Snyder C, Zhou L, Dong Y, Charman W.N, Matile H, Urwyler H, Dorn A, Vennerstrom J.L. The comparative antimalarial properties of weak base and neutral synthetic ozonides. Bioorg Med Chem Lett. 2010;20(2):563-566. DOI: 10.1016/j.bmcl.2009.11.088

Wang X, Creek D.J, Schiaffo C.E, Dong Y, Chollet J, Scheurer C, Wittlin S, Charman S.A, Dussault P.H, Wood J.K, Vennerstrom J.L. Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs: relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity. Bioorg Med Chem Lett. 2009;19(16):4542-4545. DOI: 10.1016/j.bmcl.2009.07.013

Hofer S, Brun R, Maerki S, Matile H, Scheurer C, Wittlin S. In vitro assessment of the pharmacodynamic properties of DB75, piperaquine, OZ277 and OZ401 in cultures of Plasmodium falciparum. J Antimicrob Chemother. 2008;62(5):1061-1064

Zhou L, Alker A, Ruf A, Wang X.F, Chiu F.C.K, Morizzi J, Charman S.A, Charman W.N, Scheurer C, Wittlin S, Dong Y.X, Hunziker D, Vennerstrom J.L. Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277. Bioorg Med Chem Lett. 2008;18(5):1555-1558. DOI: 10.1016/j.bmcl.2008.01.087

Osorio L, Murillo C, Aponte S, Mayagaya V, Scheurer C, Brun R, Matile H, Wittlin S. In vitro susceptibility of P. falciparum populations from Colombia and Tanzania to a new synthetic peroxide (OZ277). Am J Trop Med Hyg. 2007;76(6):1024-1026

Snyder C, Chollet J, Santo-Tomas J, Scheurer C, Wittlin S. In vitro and in vivo interaction of synthetic peroxide RBx11160 (OZ277) with piperaquine in Plasmodium models. Exp Parasitol. 2007;115(3):296-300

Wang X, Dong Y, Wittlin S, Creek D, Chollet J, Charman S.A, Tomas J.S, Scheurer C, Snyder C, Vennerstrom J.L. Spiro- and dispiro-1,2-dioxolanes: contribution of iron(II)-mediated one-electron vs two-electron reduction to the activity of antimalarial peroxides. J Med Chem. 2007;50(23):5840-5847

Dong Y, Tang Y, Chollet J, Matile H, Wittlin S, Charman S.A, Charman W.N, Santo Tomas J, Scheurer C, Snyder C, Scorneaux B, Bajpai S, Alexander S.A, Wang X, Padmanilayam M, Cheruku S.R, Brun R, Vennerstrom J.L. Effect of functional group polarity on the antimalarial activity of spiro and dispiro-1,2,4-trioxolanes. Bioorg Med Chem Lett. 2006;14:6368-6382. DOI: 10.1016/j.bmc.2006.05.041

Kocken C.H.M, Van der Wel A, Arbe-Barnes S, Brun R, Matile H, Scheurer C, Wittlin S, Thomas A.W. Plasmodium vivax : in vitro susceptibility of blood stages to synthetic trioxolane compounds and the diamidine DB75. Exp Parasitol. 2006;113:197-200

Padmanilayam M, Scorneaux B, Dong Y, Chollet J, Matile H, Charman S.A, Creek D.J, Charman W.N, Tomas J.S, Scheurer C, Wittlin S, Brun R, Vennerstrom J.L. Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine. Bioorg Med Chem Lett. 2006;16(21):5542-5545

Dong Y, Chollet J, Matile H, Charman S.A, Chiu F.C, Charman W.N, Scorneaux B, Urwyler H, Santo Tomas J, Scheurer C, Snyder C, Dorn A, Wang X, Karle J.M, Tang Y, Wittlin S, Brun R, Vennerstrom J.L. Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes. J Med Chem. 2005;48(15):4953-4961

Vennerstrom J.L, Brun R, Charman S.A, Chiu F, Chollet J, Dong Y, Dorn A, Hunziker D, Matile H, McIntosh K, Padmanilayam M, Santo Tomas J, Scheurer C, Scorneaux B, Tang J, Urwyler H, Wittlin S, Charman W.N. Novel antimalarial peroxides: Identification of a trioxolane drug development candidate. Nature. 2004;430:900-904