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Ultra-low-density Plasmodium falciparum infections in African settings.

Awandu SS, Raman J, Bousema T, Birkholtz LM.

Clin Infect Dis. 2019 Feb 15. pii: ciz147. doi: 10.1093/cid/ciz147. [Epub ahead of print] No abstract available.


Structure-activity relationship studies and Plasmodium life cycle profiling identifies pan-active N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazoles which are efficacious in an in vivo mouse model of malaria.

Mayoka G, Njoroge M, Okombo J, Gibhard L, Sanches-Vaz M, Fontinha D, Birkholtz LM, Reader J, van der Watt M, Coetzer TL, Lauterbach S, Churchyard A, Bezuidenhout B, Egan TJ, Yeates CL, Wittlin S, Prudêncio M, Chibale K.

J Med Chem. 2018 Dec 18. doi: 10.1021/acs.jmedchem.8b01769. [Epub ahead of print]


Multistage Antiplasmodium Activity of Astemizole Analogues and Inhibition of Hemozoin Formation as a Contributor to Their Mode of Action.

Kumar M, Okombo J, Mambwe D, Taylor D, Lawrence N, Reader J, van der Watt M, Fontinha D, Sanches-Vaz M, Bezuidenhout BC, Lauterbach SB, Liebenberg D, Birkholtz LM, Coetzer TL, Prudêncio M, Egan TJ, Wittlin S, Chibale K.

ACS Infect Dis. 2019 Feb 8;5(2):303-315. doi: 10.1021/acsinfecdis.8b00272. Epub 2019 Jan 7.


Inducing controlled cell cycle arrest and re-entry during asexual proliferation of Plasmodium falciparum malaria parasites.

van Biljon R, Niemand J, van Wyk R, Clark K, Verlinden B, Abrie C, von Grüning H, Smidt W, Smit A, Reader J, Painter H, Llinás M, Doerig C, Birkholtz LM.

Sci Rep. 2018 Nov 8;8(1):16581. doi: 10.1038/s41598-018-34964-w.


Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. No abstract available.


Synthesis, antimalarial activities and cytotoxicities of amino-artemisinin-1,2-disubstituted ferrocene hybrids.

de Lange C, Coertzen D, Smit FJ, Wentzel JF, Wong HN, Birkholtz LM, Haynes RK, N'Da DD.

Bioorg Med Chem Lett. 2018 Oct 15;28(19):3161-3163. doi: 10.1016/j.bmcl.2018.08.037. Epub 2018 Aug 28.


UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Erratum in: Antimicrob Agents Chemother. 2018 Oct 24;62(11):.


Artemisone and Artemiside Are Potent Panreactive Antimalarial Agents That Also Synergize Redox Imbalance in Plasmodium falciparum Transmissible Gametocyte Stages.

Coertzen D, Reader J, van der Watt M, Nondaba SH, Gibhard L, Wiesner L, Smith P, D'Alessandro S, Taramelli D, Wong HN, du Preez JL, Wu RWK, Birkholtz LM, Haynes RK.

Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e02214-17. doi: 10.1128/AAC.02214-17. Print 2018 Aug.


Understanding human genetic factors influencing primaquine safety and efficacy to guide primaquine roll-out in a pre-elimination setting in southern Africa.

Awandu SS, Raman J, Makhanthisa TI, Kruger P, Frean J, Bousema T, Niemand J, Birkholtz LM.

Malar J. 2018 Mar 20;17(1):120. doi: 10.1186/s12936-018-2271-z.


Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials.

van der Watt ME, Reader J, Churchyard A, Nondaba SH, Lauterbach SB, Niemand J, Abayomi S, van Biljon RA, Connacher JI, van Wyk RDJ, Le Manach C, Paquet T, González Cabrera D, Brunschwig C, Theron A, Lozano-Arias S, Rodrigues JFI, Herreros E, Leroy D, Duffy J, Street LJ, Chibale K, Mancama D, Coetzer TL, Birkholtz LM.

J Antimicrob Chemother. 2018 May 1;73(5):1279-1290. doi: 10.1093/jac/dky008.


Synthesis, in vitro antimalarial activities and cytotoxicities of amino-artemisinin-ferrocene derivatives.

de Lange C, Coertzen D, Smit FJ, Wentzel JF, Wong HN, Birkholtz LM, Haynes RK, N'Da DD.

Bioorg Med Chem Lett. 2017 Dec 26. pii: S0960-894X(17)31231-3. doi: 10.1016/j.bmcl.2017.12.057. [Epub ahead of print]


Activities of 11-Azaartemisinin and N-Sulfonyl Derivatives against Asexual and Transmissible Malaria Parasites.

Harmse R, Coertzen D, Wong HN, Smit FJ, van der Watt ME, Reader J, Nondaba SH, Birkholtz LM, Haynes RK, N'Da DD.

ChemMedChem. 2017 Dec 19;12(24):2086-2093. doi: 10.1002/cmdc.201700599. Epub 2017 Dec 8.


Preliminary Evaluation of Artemisinin-Cholesterol Conjugates as Potential Drugs for the Treatment of Intractable Forms of Malaria and Tuberculosis.

Morake M, Coertzen D, Ngwane A, Wentzel JF, Wong HN, Smit FJ, Birkholtz LM, Pietersen RD, Baker B, Wiid I, N'Da DD, Haynes RK.

ChemMedChem. 2018 Jan 8;13(1):67-77. doi: 10.1002/cmdc.201700579. Epub 2017 Dec 15.


Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ, Bantscheff M, Ruecker A, Blagborough AM, Zakutansky SE, Zeeman AM, White KL, Shackleford DM, Mannila J, Morizzi J, Scheurer C, Angulo-Barturen I, Martínez MS, Ferrer S, Sanz LM, Gamo FJ, Reader J, Botha M, Dechering KJ, Sauerwein RW, Tungtaeng A, Vanachayangkul P, Lim CS, Burrows J, Witty MJ, Marsh KC, Bodenreider C, Rochford R, Solapure SM, Jiménez-Díaz MB, Wittlin S, Charman SA, Donini C, Campo B, Birkholtz LM, Hanson KK, Drewes G, Kocken CHM, Delves MJ, Leroy D, Fidock DA, Waterson D, Street LJ, Chibale K.

Sci Transl Med. 2017 Apr 26;9(387). pii: eaad9735. doi: 10.1126/scitranslmed.aad9735.


Quantitative chromatin proteomics reveals a dynamic histone post-translational modification landscape that defines asexual and sexual Plasmodium falciparum parasites.

Coetzee N, Sidoli S, van Biljon R, Painter H, Llinás M, Garcia BA, Birkholtz LM.

Sci Rep. 2017 Apr 4;7(1):607. doi: 10.1038/s41598-017-00687-7.


Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.

Singh K, Okombo J, Brunschwig C, Ndubi F, Barnard L, Wilkinson C, Njogu PM, Njoroge M, Laing L, Machado M, Prudêncio M, Reader J, Botha M, Nondaba S, Birkholtz LM, Lauterbach S, Churchyard A, Coetzer TL, Burrows JN, Yeates C, Denti P, Wiesner L, Egan TJ, Wittlin S, Chibale K.

J Med Chem. 2017 Feb 23;60(4):1432-1448. doi: 10.1021/acs.jmedchem.6b01641. Epub 2017 Feb 7.


Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.

Le Manach C, Nchinda AT, Paquet T, Gonzàlez Cabrera D, Younis Y, Han Z, Bashyam S, Zabiulla M, Taylor D, Lawrence N, White KL, Charman SA, Waterson D, Witty MJ, Wittlin S, Botha ME, Nondaba SH, Reader J, Birkholtz LM, Jiménez-Díaz MB, Martínez MS, Ferrer S, Angulo-Barturen I, Meister S, Antonova-Koch Y, Winzeler EA, Street LJ, Chibale K.

J Med Chem. 2016 Nov 10;59(21):9890-9905. Epub 2016 Oct 26.


Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities.

Beteck RM, Coertzen D, Smit FJ, Birkholtz LM, Haynes RK, N'Da DD.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):3006-3009. doi: 10.1016/j.bmcl.2016.05.024. Epub 2016 May 9.


Discovering New Transmission-Blocking Antimalarial Compounds: Challenges and Opportunities.

Birkholtz LM, Coetzer TL, Mancama D, Leroy D, Alano P.

Trends Parasitol. 2016 Sep;32(9):669-681. doi: 10.1016/ Epub 2016 May 18. Review.


Use of a Chimeric Hsp70 to Enhance the Quality of Recombinant Plasmodium falciparum S-Adenosylmethionine Decarboxylase Protein Produced in Escherichia coli.

Makhoba XH, Burger A, Coertzen D, Zininga T, Birkholtz LM, Shonhai A.

PLoS One. 2016 Mar 31;11(3):e0152626. doi: 10.1371/journal.pone.0152626. eCollection 2016.


In vitro inhibition of Plasmodium falciparum early and late stage gametocyte viability by extracts from eight traditionally used South African plant species.

Moyo P, Botha ME, Nondaba S, Niemand J, Maharaj VJ, Eloff JN, Louw AI, Birkholtz L.

J Ethnopharmacol. 2016 Jun 5;185:235-42. doi: 10.1016/j.jep.2016.03.036. Epub 2016 Mar 16.


Resisting resistance: is there a solution for malaria?

Verlinden BK, Louw A, Birkholtz LM.

Expert Opin Drug Discov. 2016;11(4):395-406. doi: 10.1517/17460441.2016.1154037. Epub 2016 Feb 29. Review.


A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.

Le Manach C, Paquet T, Brunschwig C, Njoroge M, Han Z, Gonzàlez Cabrera D, Bashyam S, Dhinakaran R, Taylor D, Reader J, Botha M, Churchyard A, Lauterbach S, Coetzer TL, Birkholtz LM, Meister S, Winzeler EA, Waterson D, Witty MJ, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Street LJ, Chibale K.

J Med Chem. 2015 Nov 12;58(21):8713-22. doi: 10.1021/acs.jmedchem.5b01605. Epub 2015 Nov 2.


Nowhere to hide: interrogating different metabolic parameters of Plasmodium falciparum gametocytes in a transmission blocking drug discovery pipeline towards malaria elimination.

Reader J, Botha M, Theron A, Lauterbach SB, Rossouw C, Engelbrecht D, Wepener M, Smit A, Leroy D, Mancama D, Coetzer TL, Birkholtz LM.

Malar J. 2015 May 22;14:213. doi: 10.1186/s12936-015-0718-z.


Morphological and Molecular Descriptors of the Developmental Cycle of Babesia divergens Parasites in Human Erythrocytes.

Rossouw I, Maritz-Olivier C, Niemand J, van Biljon R, Smit A, Olivier NA, Birkholtz LM.

PLoS Negl Trop Dis. 2015 May 8;9(5):e0003711. doi: 10.1371/journal.pntd.0003711. eCollection 2015 May.


A 2-methoxyestradiol bis-sulphamoylated derivative induces apoptosis in breast cell lines.

Visagie MH, Birkholtz LM, Joubert AM.

Cell Biosci. 2015 Apr 22;5:19. doi: 10.1186/s13578-015-0010-5. eCollection 2015.


Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites.

Verlinden BK, de Beer M, Pachaiyappan B, Besaans E, Andayi WA, Reader J, Niemand J, van Biljon R, Guy K, Egan T, Woster PM, Birkholtz LM.

Bioorg Med Chem. 2015 Aug 15;23(16):5131-43. doi: 10.1016/j.bmc.2015.01.036. Epub 2015 Jan 28.


A novel inhibitor of Plasmodium falciparum spermidine synthase: a twist in the tail.

Burger PB, Williams M, Sprenger J, Reeksting SB, Botha M, Müller IB, Joubert F, Birkholtz LM, Louw AI.

Malar J. 2015 Feb 5;14:54. doi: 10.1186/s12936-015-0572-z.


Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters.

Smit FJ, van Biljon RA, Birkholtz LM, N'Da DD.

Eur J Med Chem. 2015 Jan 27;90:33-44. doi: 10.1016/j.ejmech.2014.11.016. Epub 2014 Nov 7.


Novel S-adenosyl-L-methionine decarboxylase inhibitors as potent antiproliferative agents against intraerythrocytic Plasmodium falciparum parasites.

le Roux D, Burger PB, Niemand J, Grobler A, Urbán P, Fernàndez-Busquets X, Barker RH, Serrano AE, I Louw A, Birkholtz LM.

Int J Parasitol Drugs Drug Resist. 2013 Dec 5;4(1):28-36. doi: 10.1016/j.ijpddr.2013.11.003. eCollection 2014 Apr.


Discovery of compounds blocking the proliferation of Toxoplasma gondii and Plasmodium falciparum in a chemical space based on piperidinyl-benzimidazolone analogs.

Saïdani N, Botté CY, Deligny M, Bonneau AL, Reader J, Lasselin R, Merer G, Niepceron A, Brossier F, Cintrat JC, Rousseau B, Birkholtz LM, Cesbron-Delauw MF, Dubremetz JF, Mercier C, Vial H, Lopez R, Maréchal E.

Antimicrob Agents Chemother. 2014 May;58(5):2586-97. doi: 10.1128/AAC.01445-13. Epub 2014 Feb 18.


17-beta-estradiol analog inhibits cell proliferation by induction of apoptosis in breast cell lines.

Visagie MH, Birkholtz LM, Joubert AM.

Microsc Res Tech. 2014 Mar;77(3):236-42. doi: 10.1002/jemt.22334. Epub 2014 Jan 22.


Anthracene-polyamine conjugates inhibit in vitro proliferation of intraerythrocytic Plasmodium falciparum parasites.

Niemand J, Burger P, Verlinden BK, Reader J, Joubert AM, Kaiser A, Louw AI, Kirk K, Phanstiel O 4th, Birkholtz LM.

Antimicrob Agents Chemother. 2013 Jun;57(6):2874-7. doi: 10.1128/AAC.00106-13. Epub 2013 Apr 1.


Sustainable malaria control: transdisciplinary approaches for translational applications.

Birkholtz LM, Bornman R, Focke W, Mutero C, de Jager C.

Malar J. 2012 Dec 26;11:431. doi: 10.1186/1475-2875-11-431. Review.


Exploring inhibition of Pdx1, a component of the PLP synthase complex of the human malaria parasite Plasmodium falciparum.

Reeksting SB, Müller IB, Burger PB, Burgos ES, Salmon L, Louw AI, Birkholtz LM, Wrenger C.

Biochem J. 2013 Jan 1;449(1):175-87. doi: 10.1042/BJ20120925.


Polyamine uptake by the intraerythrocytic malaria parasite, Plasmodium falciparum.

Niemand J, Louw AI, Birkholtz L, Kirk K.

Int J Parasitol. 2012 Sep;42(10):921-9. doi: 10.1016/j.ijpara.2012.07.005. Epub 2012 Aug 2.


Inhibition of p-aminobenzoate and folate syntheses in plants and apicomplexan parasites by natural product rubreserine.

Camara D, Bisanz C, Barette C, Van Daele J, Human E, Barnard B, Van der Straeten D, Stove CP, Lambert WE, Douce R, Maréchal E, Birkholtz LM, Cesbron-Delauw MF, Dumas R, Rébeillé F.

J Biol Chem. 2012 Jun 22;287(26):22367-76. doi: 10.1074/jbc.M112.365833. Epub 2012 May 10.


Thermo-responsive non-woven scaffolds for "smart" 3D cell culture.

Rossouw CL, Chetty A, Moolman FS, Birkholtz LM, Hoppe H, Mancama DT.

Biotechnol Bioeng. 2012 Aug;109(8):2147-58. doi: 10.1002/bit.24469. Epub 2012 Feb 24.


Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities.

Verlinden BK, Niemand J, Snyman J, Sharma SK, Beattie RJ, Woster PM, Birkholtz LM.

J Med Chem. 2011 Oct 13;54(19):6624-33. doi: 10.1021/jm200463z. Epub 2011 Sep 14.


Polyamine homoeostasis as a drug target in pathogenic protozoa: peculiarities and possibilities.

Birkholtz LM, Williams M, Niemand J, Louw AI, Persson L, Heby O.

Biochem J. 2011 Sep 1;438(2):229-44. doi: 10.1042/BJ20110362. Review.


Biochemical characterisation and novel classification of monofunctional S-adenosylmethionine decarboxylase of Plasmodium falciparum.

Williams M, Sprenger J, Human E, Al-Karadaghi S, Persson L, Louw AI, Birkholtz LM.

Mol Biochem Parasitol. 2011 Nov;180(1):17-26. doi: 10.1016/j.molbiopara.2011.07.004. Epub 2011 Jul 22.


Plasmodium falciparum spermidine synthase inhibition results in unique perturbation-specific effects observed on transcript, protein and metabolite levels.

Becker JV, Mtwisha L, Crampton BG, Stoychev S, van Brummelen AC, Reeksting S, Louw AI, Birkholtz LM, Mancama DT.

BMC Genomics. 2010 Apr 12;11:235. doi: 10.1186/1471-2164-11-235.


Proteomic profiling of Plasmodium falciparum through improved, semiquantitative two-dimensional gel electrophoresis.

Smit S, Stoychev S, Louw AI, Birkholtz LM.

J Proteome Res. 2010 May 7;9(5):2170-81. doi: 10.1021/pr9009244.


Functional consequences of perturbing polyamine metabolism in the malaria parasite, Plasmodium falciparum.

Clark K, Niemand J, Reeksting S, Smit S, van Brummelen AC, Williams M, Louw AI, Birkholtz L.

Amino Acids. 2010 Feb;38(2):633-44. doi: 10.1007/s00726-009-0424-7. Epub 2009 Dec 9. Review.


Antimalarial drug discovery: in silico structural biology and rational drug design.

de Beer TA, Wells GA, Burger PB, Joubert F, Marechal E, Birkholtz L, Louw AI.

Infect Disord Drug Targets. 2009 Jun;9(3):304-18. Review.


Co-inhibition of Plasmodium falciparum S-adenosylmethionine decarboxylase/ornithine decarboxylase reveals perturbation-specific compensatory mechanisms by transcriptome, proteome, and metabolome analyses.

van Brummelen AC, Olszewski KL, Wilinski D, Llinás M, Louw AI, Birkholtz LM.

J Biol Chem. 2009 Feb 13;284(7):4635-46. doi: 10.1074/jbc.M807085200. Epub 2008 Dec 10.


Heterologous expression of plasmodial proteins for structural studies and functional annotation.

Birkholtz LM, Blatch G, Coetzer TL, Hoppe HC, Human E, Morris EJ, Ngcete Z, Oldfield L, Roth R, Shonhai A, Stephens L, Louw AI.

Malar J. 2008 Oct 1;7:197. doi: 10.1186/1475-2875-7-197. Review.


Transcriptional responses of Plasmodium falciparum to alpha-difluoromethylornithine-induced polyamine depletion.

Clark K, Dhoogra M, Louw AI, Birkholtz LM.

Biol Chem. 2008 Feb;389(2):111-25. doi: 10.1515/BC.2008.014.


Exploring functional genomics for drug target and therapeutics discovery in Plasmodia.

Birkholtz L, van Brummelen AC, Clark K, Niemand J, Maréchal E, Llinás M, Louw AI.

Acta Trop. 2008 Feb;105(2):113-23. Epub 2007 Nov 12. Review.


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