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Lyn-Marie Birkholtz

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Citations 1103
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Recent Articles
1.
Godinez-Macias K, Chen D, Wallis J, Siegel M, Adam A, Bopp S, et al.
NPJ Drug Discov . 2025 Mar; 2(1):3. PMID: 40066064
Identification of novel drug targets is a key component of modern drug discovery. While antimalarial targets are often identified through the mechanism of action studies on phenotypically derived inhibitors, this...
2.
Xie S, Tai C, Morton C, Ma L, Huang S, Wittlin S, et al.
PLoS Pathog . 2024 Dec; 20(12):e1012429. PMID: 39652589
The Plasmodium falciparum cytoplasmic tyrosine tRNA synthetase (PfTyrRS) is an attractive drug target that is susceptible to reaction-hijacking by AMP-mimicking nucleoside sulfamates. We previously identified an exemplar pyrazolopyrimidine ribose sulfamate,...
3.
Godinez-Macias K, Chen D, Wallis J, Siegel M, Adam A, Bopp S, et al.
Res Sq . 2024 Dec; PMID: 39649165
The identification of novel drug targets for the purpose of designing small molecule inhibitors is key component to modern drug discovery. In malaria parasites, discoveries of antimalarial targets have primarily...
4.
Gomez-Gonzalez P, Gupta A, Drought L, Patel A, Okombo J, van der Watt M, et al.
Sci Adv . 2024 Dec; 10(49):eadq1383. PMID: 39642214
Cyclic nucleotide-dependent phosphodiesterases (PDEs) play essential roles in regulating the malaria parasite life cycle, suggesting that they may be promising antimalarial drug targets. PDE inhibitors are used safely to treat...
5.
Naude M, van Heerden A, Reader J, van der Watt M, Niemand J, Joubert D, et al.
Nat Commun . 2024 Nov; 15(1):9896. PMID: 39548094
Novel antimalarial compounds targeting both the pathogenic and transmissible stages of the human malaria parasite, Plasmodium falciparum, would greatly benefit malaria elimination strategies. However, most compounds affecting asexual blood stage...
6.
Watson S, van der Watt M, Theron A, Reader J, Tshabalala S, Erlank E, et al.
ACS Infect Dis . 2024 Aug; 10(9):3358-3367. PMID: 39143042
Toward repositioning the antitubercular clinical candidate SQ109 as an antimalarial, analogs were investigated for structure-activity relationships for activity against asexual blood stages of the human malaria parasite pathogenic forms, as...
7.
Dziwornu G, Seanego D, Fienberg S, Clements M, Ferreira J, Sypu V, et al.
J Med Chem . 2024 Jun; 67(13):11401-11420. PMID: 38918002
Structure-activity relationship studies of 2,8-disubstituted-1,5-naphthyridines, previously reported as potent inhibitors of () phosphatidylinositol-4-kinase β (PI4K), identified 1,5-naphthyridines with basic groups at 8-position, which retained PI4K inhibitory activity but switched primary...
8.
Mbaba M, Golding T, Omondi R, Mohunlal R, Egan T, Reader J, et al.
Eur J Med Chem . 2024 Apr; 271:116429. PMID: 38663284
Amodiaquine (AQ) is a potent antimalarial drug used in combination with artesunate as part of artemisinin-based combination therapies (ACTs) for malarial treatment. Due to the rising emergence of resistant malaria...
9.
Mambwe D, Coertzen D, Leshabane M, Mulubwa M, Njoroge M, Gibhard L, et al.
ACS Med Chem Lett . 2024 Apr; 15(4):463-469. PMID: 38628794
Toward addressing the cardiotoxicity liability associated with the antimalarial drug astemizole (AST, hERG IC = 0.0042 μM) and its derivatives, we designed and synthesized analogues based on compound ( NF54...
10.
Gwarinda H, Tessema S, Raman J, Greenhouse B, Birkholtz L
Front Epidemiol . 2024 Mar; 3:1227071. PMID: 38455947
To accelerate malaria elimination in the Southern African region by 2030, it is essential to prevent cross-border malaria transmission. However, countries within the region are highly interconnected due to human...