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302 results

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Page 1
Mixed Alkyl/Aryl Phosphonates Identify Metabolic Serine Hydrolases as Antimalarial Targets.
Bennett JM, Narwal SK, Kabeche S, Abegg D, Hackett F, Yeo T, Li VL, Muir RK, Faucher FF, Lovell S, Blackman MJ, Adibekian A, Yeh E, Fidock DA, Bogyo M. Bennett JM, et al. Among authors: fidock da. bioRxiv [Preprint]. 2024 Jan 11:2024.01.11.575224. doi: 10.1101/2024.01.11.575224. bioRxiv. 2024. Update in: Cell Chem Biol. 2024 Sep 19;31(9):1714-1728.e10. doi: 10.1016/j.chembiol.2024.07.006 PMID: 38260474 Free PMC article. Updated. Preprint.
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: fidock da. J Med Chem. 2024 Dec 26. doi: 10.1021/acs.jmedchem.4c01465. Online ahead of print. J Med Chem. 2024. PMID: 39723908
Safety, tolerability, pharmacokinetics, and antimalarial activity of MMV533: a phase 1a first-in-human, randomised, ascending dose and food effect study, and a phase 1b Plasmodium falciparum volunteer infection study.
Bestgen B, Jones S, Thathy V, Kuemmerle A, Barcelo C, Haouala A, Gossen D, Marx MW, Di Resta I, Szramowska M, Webster RA, Llewellyn S, Ritacco DA, Yeo T, Leroy D, Barber BE, Fidock DA, Griffin P, Lickliter J, Chalon S. Bestgen B, et al. Among authors: fidock da. Lancet Infect Dis. 2024 Dec 18:S1473-3099(24)00664-9. doi: 10.1016/S1473-3099(24)00664-9. Online ahead of print. Lancet Infect Dis. 2024. PMID: 39708824 Free article.
Regional action needed to halt antimalarial drug resistance in Africa.
Martinez-Vega R, Ishengoma DS, Gosling R, Rosenthal PJ, Dondorp A, Barnes KI, Nsanzabana C, Djimde AA, Ochola-Oyier LI, Tibenderana J, Chimumbwa J, Golassa L, Kapologwe NA, Mbacham WF, Kamya MR, Fidock DA, Komatsu R, von Seidlein L, Dhorda M. Martinez-Vega R, et al. Among authors: fidock da. Lancet. 2024 Dec 11:S0140-6736(24)02706-5. doi: 10.1016/S0140-6736(24)02706-5. Online ahead of print. Lancet. 2024. PMID: 39674185 No abstract available.
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: fidock da. 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.
Revisiting the Plasmodium falciparum druggable genome using predicted structures and data mining.
Godinez-Macias KP, Chen D, Wallis JL, Siegel MG, Adam A, Bopp S, Carolino K, Coulson LB, Durst G, Thathy V, Esherick L, Farringer MA, Flannery EL, Forte B, Liu T, Magalhaes LG, Gupta AK, Istvan ES, Jiang T, Kumpornsin K, Lobb K, McLean K, Moura IMR, Okombo J, Payne NC, Plater A, Rao SPS, Siqueira-Neto JL, Somsen BA, Summers RL, Zhang R, Gilson MK, Gamo FJ, Campo B, Baragaña B, Duffy J, Gilbert IH, Lukens AK, Dechering KJ, Niles JC, McNamara CW, Cheng X, Birkholtz LM, Bronkhorst AW, Fidock DA, Wirth DF, Goldberg DE, Lee MCS, Winzeler EA. Godinez-Macias KP, et al. Among authors: fidock da. Res Sq [Preprint]. 2024 Nov 26:rs.3.rs-5412515. doi: 10.21203/rs.3.rs-5412515/v1. Res Sq. 2024. PMID: 39649165 Free PMC article. Preprint.
Inhibitors of malaria parasite cyclic nucleotide phosphodiesterases block asexual blood-stage development and mosquito transmission.
Gomez-Gonzalez PJ, Gupta A, Drought LG, Patel A, Okombo J, van der Watt M, Walker-Gray R, Schindler KA, Burkhard AY, Yeo T, Narwal SK, Bloxham TS, Flueck C, Walker EM, Rey JA, Fairhurst KJ, Reader J, Park H, Pollard HG, Stewart LB, Brandner-Garrod L, Kristan M, Sterk GJ, van Nuland YM, Manko E, van Schalkwyk DA, Zheng Y, Leurs R, Dechering KJ, Aguiar ACC, Guido RVC, Pereira DB, Tumwebaze PK, Nosbya SL, Rosenthal PJ, Cooper RA, Palmer M, Parkinson T, Burrows JN, Uhlemann AC, Birkholtz LM, Small-Saunders JL, Duffy J, Fidock DA, Brown A, Gardner M, Baker DA. Gomez-Gonzalez PJ, et al. Among authors: fidock da. Sci Adv. 2024 Dec 6;10(49):eadq1383. doi: 10.1126/sciadv.adq1383. Epub 2024 Dec 6. Sci Adv. 2024. PMID: 39642214 Free PMC article.
Systematic in vitro evolution in Plasmodium falciparum reveals key determinants of drug resistance.
Luth MR, Godinez-Macias KP, Chen D, Okombo J, Thathy V, Cheng X, Daggupati S, Davies H, Dhingra SK, Economy JM, Edgar RCS, Gomez-Lorenzo MG, Istvan ES, Jado JC, LaMonte GM, Melillo B, Mok S, Narwal SK, Ndiaye T, Ottilie S, Palomo Diaz S, Park H, Peña S, Rocamora F, Sakata-Kato T, Small-Saunders JL, Summers RL, Tumwebaze PK, Vanaerschot M, Xia G, Yeo T, You A, Gamo FJ, Goldberg DE, Lee MCS, McNamara CW, Ndiaye D, Rosenthal PJ, Schreiber SL, Serra G, De Siqueira-Neto JL, Skinner-Adams TS, Uhlemann AC, Kato N, Lukens AK, Wirth DF, Fidock DA, Winzeler EA. Luth MR, et al. Among authors: fidock da. Science. 2024 Nov 29;386(6725):eadk9893. doi: 10.1126/science.adk9893. Epub 2024 Nov 29. Science. 2024. PMID: 39607932
302 results