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Page 1
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: birkholtz lm. 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: birkholtz lm. 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: birkholtz lm. 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.
The Tuberculosis Drug Candidate SQ109 and Its Analogs Have Multistage Activity against Plasmodium falciparum.
Watson SJ, van der Watt ME, Theron A, Reader J, Tshabalala S, Erlank E, Koekemoer LL, Naude M, Stampolaki M, Adewole F, Sadowska K, Pérez-Lozano P, Turcu AL, Vázquez S, Ko J, Mazurek B, Singh D, Malwal SR, Njoroge M, Chibale K, Onajole OK, Kolocouris A, Oldfield E, Birkholtz LM. Watson SJ, et al. Among authors: birkholtz lm. ACS Infect Dis. 2024 Sep 13;10(9):3358-3367. doi: 10.1021/acsinfecdis.4c00461. Epub 2024 Aug 14. ACS Infect Dis. 2024. PMID: 39143042 Free PMC article.
2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy.
Dziwornu GA, Seanego D, Fienberg S, Clements M, Ferreira J, Sypu VS, Samanta S, Bhana AD, Korkor CM, Garnie LF, Teixeira N, Wicht KJ, Taylor D, Olckers R, Njoroge M, Gibhard L, Salomane N, Wittlin S, Mahato R, Chakraborty A, Sevilleno N, Coyle R, Lee MCS, Godoy LC, Pasaje CF, Niles JC, Reader J, van der Watt M, Birkholtz LM, Bolscher JM, de Bruijni MHC, Coulson LB, Basarab GS, Ghorpade SR, Chibale K. Dziwornu GA, et al. Among authors: birkholtz lm. J Med Chem. 2024 Jul 11;67(13):11401-11420. doi: 10.1021/acs.jmedchem.4c01154. Epub 2024 Jun 25. J Med Chem. 2024. PMID: 38918002 Free PMC article.
hERG, Plasmodium Life Cycle, and Cross Resistance Profiling of New Azabenzimidazole Analogues of Astemizole.
Mambwe D, Coertzen D, Leshabane M, Mulubwa M, Njoroge M, Gibhard L, Girling G, Wicht KJ, Lee MCS, Wittlin S, Moreira DRM, Birkholtz LM, Chibale K. Mambwe D, et al. Among authors: birkholtz lm. ACS Med Chem Lett. 2024 Mar 18;15(4):463-469. doi: 10.1021/acsmedchemlett.3c00496. eCollection 2024 Apr 11. ACS Med Chem Lett. 2024. PMID: 38628794 Free PMC article.
100 results