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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: koolen kmj. 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.
Replenishing the malaria drug discovery pipeline: Screening and hit evaluation of the MMV Hit Generation Library 1 (HGL1) against asexual blood stage Plasmodium falciparum, using a nano luciferase reporter read-out.
Dechering KJ, Timmerman M, Rensen K, Koolen KMJ, Honarnejad S, Vos MW, Huijs T, Henderson RWM, Chenu E, Laleu B, Montefiore BC, Segall MD, Mills JEJ, Guantai EM, Duffy J, Duffey M. Dechering KJ, et al. Among authors: koolen kmj. SLAS Discov. 2022 Sep;27(6):337-348. doi: 10.1016/j.slasd.2022.07.002. Epub 2022 Jul 21. SLAS Discov. 2022. PMID: 35872229 Free article.
Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183.
de Vries LE, Jansen PAM, Barcelo C, Munro J, Verhoef JMJ, Pasaje CFA, Rubiano K, Striepen J, Abla N, Berning L, Bolscher JM, Demarta-Gatsi C, Henderson RWM, Huijs T, Koolen KMJ, Tumwebaze PK, Yeo T, Aguiar ACC, Angulo-Barturen I, Churchyard A, Baum J, Fernández BC, Fuchs A, Gamo FJ, Guido RVC, Jiménez-Diaz MB, Pereira DB, Rochford R, Roesch C, Sanz LM, Trevitt G, Witkowski B, Wittlin S, Cooper RA, Rosenthal PJ, Sauerwein RW, Schalkwijk J, Hermkens PHH, Bonnert RV, Campo B, Fidock DA, Llinás M, Niles JC, Kooij TWA, Dechering KJ. de Vries LE, et al. Among authors: koolen kmj. Nat Commun. 2022 Apr 20;13(1):2158. doi: 10.1038/s41467-022-29688-5. Nat Commun. 2022. PMID: 35444200 Free PMC article.
Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in Plasmodium falciparum.
Schalkwijk J, Allman EL, Jansen PAM, de Vries LE, Verhoef JMJ, Jackowski S, Botman PNM, Beuckens-Schortinghuis CA, Koolen KMJ, Bolscher JM, Vos MW, Miller K, Reeves SA, Pett H, Trevitt G, Wittlin S, Scheurer C, Sax S, Fischli C, Angulo-Barturen I, Jiménez-Diaz MB, Josling G, Kooij TWA, Bonnert R, Campo B, Blaauw RH, Rutjes FPJT, Sauerwein RW, Llinás M, Hermkens PHH, Dechering KJ. Schalkwijk J, et al. Among authors: koolen kmj. Sci Transl Med. 2019 Sep 18;11(510):eaas9917. doi: 10.1126/scitranslmed.aas9917. Sci Transl Med. 2019. PMID: 31534021
A P. falciparum NF54 Reporter Line Expressing mCherry-Luciferase in Gametocytes, Sporozoites, and Liver-Stages.
Marin-Mogollon C, Salman AM, Koolen KMJ, Bolscher JM, van Pul FJA, Miyazaki S, Imai T, Othman AS, Ramesar J, van Gemert GJ, Kroeze H, Chevalley-Maurel S, Franke-Fayard B, Sauerwein RW, Hill AVS, Dechering KJ, Janse CJ, Khan SM. Marin-Mogollon C, et al. Among authors: koolen kmj. Front Cell Infect Microbiol. 2019 Apr 16;9:96. doi: 10.3389/fcimb.2019.00096. eCollection 2019. Front Cell Infect Microbiol. 2019. PMID: 31058097 Free PMC article.
Repurposing isoxazoline veterinary drugs for control of vector-borne human diseases.
Miglianico M, Eldering M, Slater H, Ferguson N, Ambrose P, Lees RS, Koolen KMJ, Pruzinova K, Jancarova M, Volf P, Koenraadt CJM, Duerr HP, Trevitt G, Yang B, Chatterjee AK, Wisler J, Sturm A, Bousema T, Sauerwein RW, Schultz PG, Tremblay MS, Dechering KJ. Miglianico M, et al. Among authors: koolen kmj. Proc Natl Acad Sci U S A. 2018 Jul 17;115(29):E6920-E6926. doi: 10.1073/pnas.1801338115. Epub 2018 Jul 2. Proc Natl Acad Sci U S A. 2018. PMID: 29967151 Free PMC article.
Diversity-oriented synthesis yields novel multistage antimalarial inhibitors.
Kato N, Comer E, Sakata-Kato T, Sharma A, Sharma M, Maetani M, Bastien J, Brancucci NM, Bittker JA, Corey V, Clarke D, Derbyshire ER, Dornan GL, Duffy S, Eckley S, Itoe MA, Koolen KM, Lewis TA, Lui PS, Lukens AK, Lund E, March S, Meibalan E, Meier BC, McPhail JA, Mitasev B, Moss EL, Sayes M, Van Gessel Y, Wawer MJ, Yoshinaga T, Zeeman AM, Avery VM, Bhatia SN, Burke JE, Catteruccia F, Clardy JC, Clemons PA, Dechering KJ, Duvall JR, Foley MA, Gusovsky F, Kocken CH, Marti M, Morningstar ML, Munoz B, Neafsey DE, Sharma A, Winzeler EA, Wirth DF, Scherer CA, Schreiber SL. Kato N, et al. Nature. 2016 Oct 20;538(7625):344-349. doi: 10.1038/nature19804. Epub 2016 Sep 7. Nature. 2016. PMID: 27602946 Free PMC article.
Salinomycin and other ionophores as a new class of antimalarial drugs with transmission-blocking activity.
D'Alessandro S, Corbett Y, Ilboudo DP, Misiano P, Dahiya N, Abay SM, Habluetzel A, Grande R, Gismondo MR, Dechering KJ, Koolen KM, Sauerwein RW, Taramelli D, Basilico N, Parapini S. D'Alessandro S, et al. Antimicrob Agents Chemother. 2015 Sep;59(9):5135-44. doi: 10.1128/AAC.04332-14. Epub 2015 Jun 8. Antimicrob Agents Chemother. 2015. PMID: 26055362 Free PMC article.
12 results