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Page 1
The Plasmodium Lactate/H+ Transporter PfFNT Is Essential and Druggable In Vivo.
Davies H, Bergmann B, Walloch P, Nerlich C, Hansen C, Wittlin S, Spielmann T, Treeck M, Beitz E. Davies H, et al. Among authors: wittlin s. Antimicrob Agents Chemother. 2023 Aug 17;67(8):e0035623. doi: 10.1128/aac.00356-23. Epub 2023 Jul 10. Antimicrob Agents Chemother. 2023. PMID: 37428074 Free PMC article.
TKK130 is a 3-Hydroxy-Propanamidine (HPA) with Potent Antimalarial In Vivo Activity and a High Barrier to Resistance.
Knaab TC, Moritz A, Pessanha de Carvalho L, Klein S, Lungerich B, Lohse K, Kruse L, Mombo-Ngoma G, Orta L, Thibaud JL, de Villiers KA, Fidock DA, Burckhardt BB, Held J, Wittlin S, Kurz T. Knaab TC, et al. Among authors: wittlin s. J Med Chem. 2025 Jan 9;68(1):95-107. doi: 10.1021/acs.jmedchem.4c01465. Epub 2024 Dec 26. J Med Chem. 2025. PMID: 39723908
A potent and selective reaction hijacking inhibitor of Plasmodium falciparum tyrosine tRNA synthetase exhibits single dose oral efficacy in vivo.
Xie SC, Tai CW, Morton CJ, Ma L, Huang SC, Wittlin S, Du Y, Hu Y, Dogovski C, Salimimarand M, Griffin R, England D, de la Cruz E, Deni I, Yeo T, Burkhard AY, Striepen J, Schindler KA, Crespo B, Gamo FJ, Khandokar Y, Hutton CA, Rabie T, Birkholtz LM, Famodimu MT, Delves MJ, Bolsher J, Koolen KMJ, van der Laak R, Aguiar ACC, Pereira DB, Guido RVC, Creek DJ, Fidock DA, Dick LR, Brand SL, Gould AE, Langston S, Griffin MDW, Tilley L. Xie SC, et al. Among authors: wittlin s. PLoS Pathog. 2024 Dec 9;20(12):e1012429. doi: 10.1371/journal.ppat.1012429. eCollection 2024 Dec. PLoS Pathog. 2024. PMID: 39652589 Free PMC article.
Addressing the Intracellular Vestibule of the Plasmodial Lactate Transporter PfFNT by p-Substituted Inhibitors Amplifies In Vitro Activity.
Nerlich C, Tiedjens F, Hertel R, Henke B, Häuer S, Panitzsch LS, Hansen K, Franck O, Mete A, Leroy D, Schade D, Peifer C, Hannus S, Becker F, Wittlin S, Spielmann T, Beitz E. Nerlich C, et al. Among authors: wittlin s. J Med Chem. 2024 Oct 24;67(20):18368-18383. doi: 10.1021/acs.jmedchem.4c01674. Epub 2024 Oct 3. J Med Chem. 2024. PMID: 39361938 Free PMC article.
Total Synthesis of Tosyl-Samroiyotmycin A and Its Biological Profiling.
Kolb B, Schmid F, Weng J, Altevogt L, Pereira Rebelo R, Wank B, Baro A, Zens A, Shekhar A, Bilitewski U, Sax S, Wittlin S, Taylor D, Müller R, Laschat S. Kolb B, et al. Among authors: wittlin s. Chemistry. 2024 Dec 18;30(71):e202403408. doi: 10.1002/chem.202403408. Epub 2024 Nov 12. Chemistry. 2024. PMID: 39348488 Free PMC article.
Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria.
Lawong A, Gahalawat S, Ray S, Ho N, Han Y, Ward KE, Deng X, Chen Z, Kumar A, Xing C, Hosangadi V, Fairhurst KJ, Tashiro K, Liszczak G, Shackleford DM, Katneni K, Chen G, Saunders J, Crighton E, Casas A, Robinson JJ, Imlay LS, Zhang X, Lemoff A, Zhao Z, Angulo-Barturen I, Jiménez-Díaz MB, Wittlin S, Campbell SF, Fidock DA, Laleu B, Charman SA, Ready JM, Phillips MA. Lawong A, et al. Among authors: wittlin s. Cell Chem Biol. 2024 Aug 15;31(8):1503-1517.e19. doi: 10.1016/j.chembiol.2024.07.001. Epub 2024 Jul 30. Cell Chem Biol. 2024. PMID: 39084225
Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3.
Calic PPS, Ashton TD, Mansouri M, Loi K, Jarman KE, Qiu D, Lehane AM, Roy S, Rao GP, Maity B, Wittlin S, Crespo B, Gamo FJ, Deni I, Fidock DA, Chowdury M, de Koning-Ward TF, Cowman AF, Jackson PF, Baud D, Brand S, Laleu B, Sleebs BE. Calic PPS, et al. Among authors: wittlin s. Eur J Med Chem. 2024 Oct 5;276:116677. doi: 10.1016/j.ejmech.2024.116677. Epub 2024 Jul 14. Eur J Med Chem. 2024. PMID: 39024967 Free article.
Chemoproteomics validates selective targeting of Plasmodium M1 alanyl aminopeptidase as an antimalarial strategy.
Giannangelo C, Challis MP, Siddiqui G, Edgar R, Malcolm TR, Webb CT, Drinkwater N, Vinh N, Macraild C, Counihan N, Duffy S, Wittlin S, Devine SM, Avery VM, De Koning-Ward T, Scammells P, McGowan S, Creek DJ. Giannangelo C, et al. Among authors: wittlin s. Elife. 2024 Jul 8;13:RP92990. doi: 10.7554/eLife.92990. Elife. 2024. PMID: 38976500 Free PMC article.
217 results