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CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs.
Ng CL, Siciliano G, Lee MC, de Almeida MJ, Corey VC, Bopp SE, Bertuccini L, Wittlin S, Kasdin RG, Le Bihan A, Clozel M, Winzeler EA, Alano P, Fidock DA. Ng CL, et al. Among authors: wittlin s. Mol Microbiol. 2016 Aug;101(3):381-93. doi: 10.1111/mmi.13397. Epub 2016 May 7. Mol Microbiol. 2016. PMID: 27073104 Free PMC article.
Identification of a new chemical class of antimalarials.
Brunner R, Aissaoui H, Boss C, Bozdech Z, Brun R, Corminboeuf O, Delahaye S, Fischli C, Heidmann B, Kaiser M, Kamber J, Meyer S, Papastogiannidis P, Siegrist R, Voss T, Welford R, Wittlin S, Binkert C. Brunner R, et al. Among authors: wittlin s. J Infect Dis. 2012 Sep 1;206(5):735-43. doi: 10.1093/infdis/jis418. Epub 2012 Jun 25. J Infect Dis. 2012. PMID: 22732921
UV-triggered affinity capture identifies interactions between the Plasmodium falciparum multidrug resistance protein 1 (PfMDR1) and antimalarial agents in live parasitized cells.
Brunner R, Ng CL, Aissaoui H, Akabas MH, Boss C, Brun R, Callaghan PS, Corminboeuf O, Fidock DA, Frame IJ, Heidmann B, Le Bihan A, Jenö P, Mattheis C, Moes S, Müller IB, Paguio M, Roepe PD, Siegrist R, Voss T, Welford RW, Wittlin S, Binkert C. Brunner R, et al. Among authors: wittlin s. J Biol Chem. 2013 Aug 2;288(31):22576-83. doi: 10.1074/jbc.M113.453159. Epub 2013 Jun 10. J Biol Chem. 2013. PMID: 23754276 Free PMC article.
In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models.
Schleiferböck S, Scheurer C, Ihara M, Itoh I, Bathurst I, Burrows JN, Fantauzzi P, Lotharius J, Charman SA, Morizzi J, Shackleford DM, White KL, Brun R, Wittlin S. Schleiferböck S, et al. Among authors: wittlin s. Drug Des Devel Ther. 2013 Nov 15;7:1377-84. doi: 10.2147/DDDT.S51298. eCollection 2013. Drug Des Devel Ther. 2013. PMID: 24255594 Free PMC article.
Identification and deconvolution of cross-resistance signals from antimalarial compounds using multidrug-resistant Plasmodium falciparum strains.
Chugh M, Scheurer C, Sax S, Bilsland E, van Schalkwyk DA, Wicht KJ, Hofmann N, Sharma A, Bashyam S, Singh S, Oliver SG, Egan TJ, Malhotra P, Sutherland CJ, Beck HP, Wittlin S, Spangenberg T, Ding XC. Chugh M, et al. Among authors: wittlin s. Antimicrob Agents Chemother. 2015 Feb;59(2):1110-8. doi: 10.1128/AAC.03265-14. Epub 2014 Dec 8. Antimicrob Agents Chemother. 2015. PMID: 25487796 Free PMC article.
A novel multiple-stage antimalarial agent that inhibits protein synthesis.
Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH. Baragaña B, et al. Among authors: wittlin s. Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Nature. 2015. PMID: 26085270 Free PMC article.
A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria.
Phillips MA, Lotharius J, Marsh K, White J, Dayan A, White KL, Njoroge JW, El Mazouni F, Lao Y, Kokkonda S, Tomchick DR, Deng X, Laird T, Bhatia SN, March S, Ng CL, Fidock DA, Wittlin S, Lafuente-Monasterio M, Benito FJ, Alonso LM, Martinez MS, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Haselden JN, Louttit J, Cui Y, Sridhar A, Zeeman AM, Kocken C, Sauerwein R, Dechering K, Avery VM, Duffy S, Delves M, Sinden R, Ruecker A, Wickham KS, Rochford R, Gahagen J, Iyer L, Riccio E, Mirsalis J, Bathhurst I, Rueckle T, Ding X, Campo B, Leroy D, Rogers MJ, Rathod PK, Burrows JN, Charman SA. Phillips MA, et al. Among authors: wittlin s. Sci Transl Med. 2015 Jul 15;7(296):296ra111. doi: 10.1126/scitranslmed.aaa6645. Sci Transl Med. 2015. PMID: 26180101 Free PMC article.
A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.
Le Manach C, Paquet T, Brunschwig C, Njoroge M, Han Z, Gonzàlez Cabrera D, Bashyam S, Dhinakaran R, Taylor D, Reader J, Botha M, Churchyard A, Lauterbach S, Coetzer TL, Birkholtz LM, Meister S, Winzeler EA, Waterson D, Witty MJ, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Street LJ, Chibale K. Le Manach C, et al. Among authors: wittlin s. J Med Chem. 2015 Nov 12;58(21):8713-22. doi: 10.1021/acs.jmedchem.5b01605. Epub 2015 Nov 2. J Med Chem. 2015. PMID: 26502160
204 results