2024 publications:

Greyling N, van der Watt M, Gwarinda H, van Heerden A, Greenhouse B, Leroy D, Niemand J, Birkholtz L-M. Genetic complexity alters drug susceptibility of asexual and gametocyte stages of Plasmodium falciparum to antimalarial candidates. Antimicrob Agents Chemother. 2024 6;68(3):e0129123. doi: 10.1128/aac.01291-23. Epub 2024 Jan 23. PMID: 38259087; PMCID: PMC10916389.

2023 publications:

van Heerden A, Turon G, Duran-Frigola M, Pillay N, Birkholtz LM. Machine Learning Approaches Identify Chemical Features for Stage-Specific Antimalarial Compounds. ACS Omega. 2023 7;8(46):43813-43826. doi: 10.1021/acsomega.3c05664. PMID: 38027377; PMCID: PMC10666252.

Mutombo Mianda S, Moyo P, Maboane S, Birkholtz LM, Maharaj VJ. Phytoconstituents from Turrea obtusifolia and their antiplasmodial activity. Nat Prod Res. 2023 15:1-13. doi: 10.1080/14786419.2023.2255921. Epub ahead of print. PMID: 37712398.

Gwarinda HB, Tessema SK, Raman J, Greenhouse B, Birkholtz LM. Population structure and genetic connectivity of Plasmodium falciparum in pre-elimination settings of Southern Africa. Front Epidemiol. 2023 1;3:1227071. doi: 10.3389/fepid.2023.1227071. PMID: 38455947; PMCID: PMC10910941.

Stampolaki, M., Malwal, S.R., Alvarez-Cabrera, N., Gao, Z., Moniruzzaman, M., Babii, S.O., Naziris, N., Rey-Cibati, A., Valladares-Delgado, M., Turcu, A.L., Baek, K.H., Phan, T.N., Lee, H., Alcaraz, M., Watson, S., van der Watt, M., Coertzen, D., Efstathiou, N., Chountoulesi, M., Shoen, C.M., Papanastasiou, I.P., Brea, J., Cynamon, M.H., Birkholtz, L.M., Kremer, L., No, J.H., Vázquez, S., Benaim, G., Demetzos, C., Zgurskaya, H.I., Dick, T., Oldfield, E., Kolocouris, A.D. Synthesis and Testing of Analogs of the Tuberculosis Drug Candidate SQ109 against Bacteria and Protozoa: Identification of Lead Compounds against Mycobacterium abscessus and Malaria Parasites. ACS Infect. Dis. 2023. doi: 10.1021/acsinfecdis.2c00537 

2022 publications:

Abacha, Y.Z., Forkuo, A.D., Gbedema, S.Y., Mittal, N., Ottile, S., Rocamora, F., Winzeler, E.A., Van Schalkwyk, D.A., Kelly, J., Taylor, M.C., Reader, J., Birkholtz, L., Lisgarten, D.R., Cockcroft, J.K., Lisgarten, J.N., Palmer, R.A., Talbert, R., Shnyder, S.D., Wright, C.W. Semi-Synthetic Analogues of Cryptolepine as a Potential Source of Sustainable Drugs for the Treatment of Malaria, Human African Trypanosomiasis and Cancer. Frontiers in Pharmacology Experimental Pharmacology and Drug Discovery. 2022; 13:875647. doi: 10.3389/fphar.2022.875647

Arendse, L.B., Murithi, J.M., Qahash, T., Pasaje, C.F.A., Godoy, L.C., Dey, S., Gibhard, L., Ghidelli-Disse, S., Drewes, G., Bantscheff, M., Lafuente-Monasterio, M.J., Fienberg, S., Wambua, L., Gachuhi, S., Coertzen, D., van der Watt, M., Reader, J., Aswat, A.S., Erlank, E., Venter, N., Mittal, N., Luth, M.R., Ottilie, S., Winzeler, E.A., Koekemoer, L.L., Birkholtz L.M., Niles, J.C., Llinás, M., Fidock, D.A., Chibale, K. The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and lifecycle stages. Science Translational Medicine. 2022; 14, eabo7219. doi: 10.1126/scitranslmed.abo7219

Birkholtz, L., Alano, P., Leroy, D. Transmission-blocking antimalarials for malaria elimination. Trends in Parasitology. 2022; S1471-4922(22)00012-5. doi: 10.1016/j.pt.2022.01.011

Connacher, J., von Grüning, H., Birkholtz, L. Histone modification landscapes as a roadmap for malaria parasite development. Frontiers Cell and Developmental Biology, Special Issue: How Epigenetic Mechanisms Contribute to Host-Parasite Interaction. 2022; 14156:37:00. doi: 10.3389/fcell.2022.848797

Maharaj, S., Ekoka, E., Erlank, E., Nardini, L., Reader, J., Birkholtz, L.M., Koekemoer, L.L. The ecdysone receptor regulates several key physiological factors in Anopheles funestus. Malar J. 2022; 21(1):97. doi: 10.1186/s12936-022-04123-8

Mambwe, D., Korkor, C., Mabhula, A., Ngqumba, Z., Cloete, C., Kumar, M., Barros, P., Leshabane, M., Coertzen, D., Taylor, D., Gibhard, L., Njoroge, M., Lawrence, N., Reader, J., Moreira, DR., Birkholtz, L., Wittlin, S., Egan, T., Chibale, K. Novel 3-Trifluoromethyl-1,2,4-Oxadiazole Analogues of Astemizole with Multi-Stage Antiplasmodium Activity and In vivo Efficacy in a Plasmodium berghei Mouse Malaria Infection Model. J Med Chem. 2022; 65(24):16695-16715. doi: 10.1021/acs.jmedchem.2c01516

Mianda, M.S, Invernizzi, L., van der Watt, M.E., Reader, J., Moyo, P., Birkholtz, L., Maharaja, V.J. In vitro dual activity of Aloe marlothii and its chemical constituents against Plasmodium falciparum asexual and sexual stage parasites. J Ethnopharmacol. 2022; 297:115551. doi: 10.1016/j.jep.2022.115551

Ng, J.P. L., Han, Y., Yang, L. J., Birkholtz, L., Coertzen, D., Wong, H.W., Haynes, R. K., Coghi, P., Wong, V. K. W. Antimalarial and antitumour activities of the steroidal quinone-methide celastrol and its combinations with artemiside, artemisone and methylene blue. Frontiers in Pharmacology, section Ethnopharmacology. 2022; 2;13:988748. doi: 10.3389/fphar.2022.988748

Olivier, T., Loots, L., Kok, M., de Villiers, M., Reader, J., Birkholtz, LM., Arnott, G.E., de Villiers, K.A. Adsorption to the surface of hemozoin crystals: Structure-based design and synthesis of new amino-phenoxazine β-hematin inhibitors. ChemMedChem. 2022; 17(10):1860-7179. doi: 10.1002/cmdc.202200139

Reader, J., Opperman, D., van der Watt, E.M., Theron, A., Leshabane, M., da Rocha, S., Turner, J., Garrabrant, K., Pina, I., Mills. C., Woster, P., and Birkholtz, L. New Transmission-Selective Antimalarial Agents through Hit-To-Lead Optimization of 2-([1,1'-biphenyl]-4-carboxamido) benzoic acid Derivatives. ChemBioChem (special edition Biological and Medicinal Chemistry in Africa). 2022; e202200427. doi:10.1002/cbic.202200427

Reader, J., van der Watt, M., Birkholtz, L. Streamlined and robust profiling of stage-specific gametocytocidal compounds against Plasmodium falciparum. Frontiers Cellular & Infection Microbiology (Parasite & Host) Special - Women in parasites. 2022; 12:926460. doi: 10.3389/fcimb.2022.926460

van der Watt, M.E., Reader, J., Birkholtz, L. Adapt or Die: targeting unique transmission-stage biology for malaria elimination. Frontiers in Cellular and Infection Microbiology (Parasite & Host) Special Women in Parasites. 2022; 12:901971. doi: 10.3389/fcimb.2022.901971

von Grüning, H., Coradin, M., Mendoza, M.R., Reader, J., Sidoli, S., Garcia, B.A. and Birkholtz, L. A dynamic and combinatorial histone code drives malaria parasite asexual and sexual development. Mol Cell Proteomics. 2022; 21(3):100199. doi: 10.1016/j.mcpro.2022.100199

2021 Publications

Cheuka PM, Centani L, Arendse LB, Fienberg S, Wambua L, Renga SS, Dziwornu GA, Kumar M, Lawrence N, Taylor D, Wittlin S, Coertzen D, Reader J, van der Watt M, Birkholtz L, Chibale K. New amidated 3, 6-Diphenylated Imidazopyridazines with potent antiplasmodium activity are dual inhibitors of Plasmodium Phosphatidylinositol-4-kinase and cGMP-dependent protein kinase. ACS Infectious Diseases. 2021;7(1):34-36. doi:10.1021/acsinfecdis.0c00481

Connacher J, Josling GA, Orchard LM, Reader J, Llinás M, Birkholtz LM. H3K36 methylation reprograms gene expression to drive early gametocyte development in Plasmodium falciparum. Epigenetics and Chromatin. 2021;14(1):1-15. doi:org/10.1186/s13072-021-00393-9

Dziwornu GA, Coertzen D, Leshabane M, Korkor CM, Cloete CK, Njoroge M, Gibhard L, Lawrence N, Reader J, van der Watt M, Wittlin S, Birkholtz LM, Chibale K. Antimalarial Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains Inhibit Microtubule and Hemozoin Formation: Structure–Activity Relationship and In Vivo Oral Efficacy Studies. Journal of Medicinal Chemistry. 2021;64(8):5198-215. doi:org/10.1021/acs.jmedchem.1c00354

Gwarinda HB, Tessema SK, Raman J, Greenhouse B, Birkholtz LM. Parasite genetic diversity reflects continued residual malaria transmission in Vhembe District, a hotspot in the Limpopo Province of South Africa. Malaria Journal. 2021;20(1):1-13. doi:org/10.1186/s12936-021-03635-z

Le Manach C, Dam J, Woodland JG, Kaur G, Khonde LP, Brunschwig C, Njoroge M, Wicht KJ, Horatscheck A, Paquet T, Boyle GA, Gibhard L, Taylor D, Lawrence N, Yeo T, Mok S, Eastman RT, Dorjsuren D, Talley DC, Guo H, Simeonov A, Reader J, van der Watt M, Erlank E, Venter N, Zawada JW, Aswat A, Nardini L, Coetzer TL, Lauterbach SB, Bezuidenhout BC, Theron A, Mancama D, Koekemoer LL, Birkholtz LM, Wittlin S, Delves M, Ottilie S, Winzeler EA, von Geldern TW, Smith D, Fidock DA, Street LJ, Basarab GS, Duffy J, Chibale K. Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts. Journal of Medicinal Chemistry. 2021;64(4):2291-309. doi:org/10.1021/acs.jmedchem.1c00034

Leshabane M, Dziwornu GA, Coertzen D, Reader J, Moyo P, van der Watt M, Chisanga K, Nsanzubuhoro C, Ferger R, Erlank E, Venter N, Koekemoer LL, Chibale K, Birkholtz LM. Benzimidazole Derivatives Are Potent against Multiple Life Cycle Stages of Plasmodium falciparum Malaria Parasites. ACS Infectious Diseases. 2021; doi.org/10.1021/acsinfecdis.0c00910

Reader J, van der Watt ME, Taylor D, Le Manach C, Mittal N, Ottilie S, Theron A, Moyo P, Erlank E, Nardini L, Venter N, Lauterbach S, Bezuidenhout B, Horatscheck A, van Heerden A, Boyle GA, Calvo D, Mancama D, Coetzer TL, Winzeler EA, Duffy J, Koekemoer LL, Basarab G, Chibale K, Birkholtz L-M. Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box. Nature Communation. 2021;12(269). doi:org/10.1038/s41467-020-20629-8

Van Heerden A, van Wyk R, Birkholtz LM. Machine Learning Uses Chemo-Transcriptomic Profiles to Stratify Antimalarial Compounds With Similar Mode of Action. Frontiers in Cellular and Infection Microbiology. 2021;11:558. doi:org/10.3389/fcimb.2021.688256

van Wyk R, van Biljon R, Birkholtz LM. MALBoost: a web-based application for gene regulatory network analysis in Plasmodium falciparum. Malaria Journal. 2021;20(1):317. doi:org/10.1186/s12936-021-03848-2

Niemand, J., van Biljon, R., van der Watt, M., van Heerden, A., Reader, J., van Wyk, R., Orchard, L., Chibale, K., Llinás, M., and Birkholtz, L. Chemogenomic fingerprints associated with stage-specific gametocytocidal compound action against human malaria parasites. 2021; 7(10):2904-2916. doi.org/10.1021/acsinfecdis.1c00373 

Mambwe D, Kumar M, Ferger R, Taylor D, Njoroge M, Coertzen D, Reader J, van der Watt M, Birkholtz LM, Chibale K. Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against Plasmodium falciparum In Vitro.