Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites
Identifieur interne : 000150 ( Pmc/Checkpoint ); précédent : 000149; suivant : 000151Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites
Auteurs : Nanika Coetzee ; Hilde Von Grüning ; Daniel Opperman ; Mariette Van Der Watt ; Janette Reader ; Lyn-Marié BirkholtzSource :
- Scientific Reports [ 2045-2322 ] ; 2020.
Abstract
The epigenome of the malaria parasite,
Url:
DOI: 10.1038/s41598-020-59298-4
PubMed: 32047203
PubMed Central: 7012883
Affiliations:
Links toward previous steps (curation, corpus...)
Links to Exploration step
PMC:7012883Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Epigenetic inhibitors target multiple stages of <italic>Plasmodium falciparum</italic>
parasites</title>
<author><name sortKey="Coetzee, Nanika" sort="Coetzee, Nanika" uniqKey="Coetzee N" first="Nanika" last="Coetzee">Nanika Coetzee</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Von Gruning, Hilde" sort="Von Gruning, Hilde" uniqKey="Von Gruning H" first="Hilde" last="Von Grüning">Hilde Von Grüning</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Opperman, Daniel" sort="Opperman, Daniel" uniqKey="Opperman D" first="Daniel" last="Opperman">Daniel Opperman</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Van Der Watt, Mariette" sort="Van Der Watt, Mariette" uniqKey="Van Der Watt M" first="Mariette" last="Van Der Watt">Mariette Van Der Watt</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Reader, Janette" sort="Reader, Janette" uniqKey="Reader J" first="Janette" last="Reader">Janette Reader</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Birkholtz, Lyn Marie" sort="Birkholtz, Lyn Marie" uniqKey="Birkholtz L" first="Lyn-Marié" last="Birkholtz">Lyn-Marié Birkholtz</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
</titleStmt>
<publicationStmt><idno type="wicri:source">PMC</idno>
<idno type="pmid">32047203</idno>
<idno type="pmc">7012883</idno>
<idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7012883</idno>
<idno type="RBID">PMC:7012883</idno>
<idno type="doi">10.1038/s41598-020-59298-4</idno>
<date when="2020">2020</date>
<idno type="wicri:Area/Pmc/Corpus">000204</idno>
<idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">000204</idno>
<idno type="wicri:Area/Pmc/Curation">000204</idno>
<idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Curation">000204</idno>
<idno type="wicri:Area/Pmc/Checkpoint">000150</idno>
<idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Checkpoint">000150</idno>
</publicationStmt>
<sourceDesc><biblStruct><analytic><title xml:lang="en" level="a" type="main">Epigenetic inhibitors target multiple stages of <italic>Plasmodium falciparum</italic>
parasites</title>
<author><name sortKey="Coetzee, Nanika" sort="Coetzee, Nanika" uniqKey="Coetzee N" first="Nanika" last="Coetzee">Nanika Coetzee</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Von Gruning, Hilde" sort="Von Gruning, Hilde" uniqKey="Von Gruning H" first="Hilde" last="Von Grüning">Hilde Von Grüning</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Opperman, Daniel" sort="Opperman, Daniel" uniqKey="Opperman D" first="Daniel" last="Opperman">Daniel Opperman</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Van Der Watt, Mariette" sort="Van Der Watt, Mariette" uniqKey="Van Der Watt M" first="Mariette" last="Van Der Watt">Mariette Van Der Watt</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Reader, Janette" sort="Reader, Janette" uniqKey="Reader J" first="Janette" last="Reader">Janette Reader</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
<author><name sortKey="Birkholtz, Lyn Marie" sort="Birkholtz, Lyn Marie" uniqKey="Birkholtz L" first="Lyn-Marié" last="Birkholtz">Lyn-Marié Birkholtz</name>
<affiliation><nlm:aff id="Aff1"></nlm:aff>
</affiliation>
</author>
</analytic>
<series><title level="j">Scientific Reports</title>
<idno type="eISSN">2045-2322</idno>
<imprint><date when="2020">2020</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
</fileDesc>
<profileDesc><textClass></textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en"><p id="Par1">The epigenome of the malaria parasite, <italic>Plasmodium falciparum</italic>
, is associated with regulation of various essential processes in the parasite including control of proliferation during asexual development as well as control of sexual differentiation. The unusual nature of the epigenome has prompted investigations into the potential to target epigenetic modulators with novel chemotypes. Here, we explored the diversity within a library of 95 compounds, active against various epigenetic modifiers in cancerous cells, for activity against multiple stages of <italic>P. falciparum</italic>
development. We show that <italic>P. falciparum</italic>
is differentially susceptible to epigenetic perturbation during both asexual and sexual development, with early stage gametocytes particularly sensitive to epi-drugs targeting both histone and non-histone epigenetic modifiers. Moreover, 5 compounds targeting histone acetylation and methylation show potent multistage activity against asexual parasites, early and late stage gametocytes, with transmission-blocking potential. Overall, these results warrant further examination of the potential antimalarial properties of these hit compounds.</p>
</div>
</front>
<back><div1 type="bibliography"><listBibl><biblStruct><analytic><author><name sortKey="Miller, Lh" uniqKey="Miller L">LH Miller</name>
</author>
<author><name sortKey="Ackerman, Hc" uniqKey="Ackerman H">HC Ackerman</name>
</author>
<author><name sortKey="Su, Xz" uniqKey="Su X">XZ Su</name>
</author>
<author><name sortKey="Wellems, Te" uniqKey="Wellems T">TE Wellems</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Burrows, Jn" uniqKey="Burrows J">JN Burrows</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Phillips, Ma" uniqKey="Phillips M">MA Phillips</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Audia, Je" uniqKey="Audia J">JE Audia</name>
</author>
<author><name sortKey="Campbell, Rm" uniqKey="Campbell R">RM Campbell</name>
</author>
</analytic>
</biblStruct>
<biblStruct></biblStruct>
<biblStruct><analytic><author><name sortKey="Dhanak, D" uniqKey="Dhanak D">D Dhanak</name>
</author>
<author><name sortKey="Jackson, P" uniqKey="Jackson P">P Jackson</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Coetzee, N" uniqKey="Coetzee N">N Coetzee</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Abel, Steven" uniqKey="Abel S">Steven Abel</name>
</author>
<author><name sortKey="Le Roch, Karine G" uniqKey="Le Roch K">Karine G Le Roch</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Gupta, Ap" uniqKey="Gupta A">AP Gupta</name>
</author>
<author><name sortKey="Bozdech, Z" uniqKey="Bozdech Z">Z Bozdech</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Duraisingh, Mt" uniqKey="Duraisingh M">MT Duraisingh</name>
</author>
<author><name sortKey="Skillman, Km" uniqKey="Skillman K">KM Skillman</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Cortes, Alfred" uniqKey="Cortes A">Alfred Cortés</name>
</author>
<author><name sortKey="Deitsch, Kirk W" uniqKey="Deitsch K">Kirk W. Deitsch</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Salcedo Amaya, Am" uniqKey="Salcedo Amaya A">AM Salcedo-Amaya</name>
</author>
<author><name sortKey="Hoeijmakers, Wa" uniqKey="Hoeijmakers W">WA Hoeijmakers</name>
</author>
<author><name sortKey="Bartfai, R" uniqKey="Bartfai R">R Bartfai</name>
</author>
<author><name sortKey="Stunnenberg, Hg" uniqKey="Stunnenberg H">HG Stunnenberg</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Trenholme, K" uniqKey="Trenholme K">K Trenholme</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Bouchut, A" uniqKey="Bouchut A">A Bouchut</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Malmquist, Na" uniqKey="Malmquist N">NA Malmquist</name>
</author>
<author><name sortKey="Moss, Ta" uniqKey="Moss T">TA Moss</name>
</author>
<author><name sortKey="Mecheri, S" uniqKey="Mecheri S">S Mecheri</name>
</author>
<author><name sortKey="Scherf, A" uniqKey="Scherf A">A Scherf</name>
</author>
<author><name sortKey="Fuchter, Mj" uniqKey="Fuchter M">MJ Fuchter</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Malmquist, Na" uniqKey="Malmquist N">NA Malmquist</name>
</author>
</analytic>
</biblStruct>
<biblStruct></biblStruct>
<biblStruct><analytic><author><name sortKey="Sundriyal, S" uniqKey="Sundriyal S">S Sundriyal</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Prusty, D" uniqKey="Prusty D">D Prusty</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Andrews, Kt" uniqKey="Andrews K">KT Andrews</name>
</author>
<author><name sortKey="Tran, Tn" uniqKey="Tran T">TN Tran</name>
</author>
<author><name sortKey="Wheatley, Nc" uniqKey="Wheatley N">NC Wheatley</name>
</author>
<author><name sortKey="Fairlie, Dp" uniqKey="Fairlie D">DP Fairlie</name>
</author>
</analytic>
</biblStruct>
<biblStruct></biblStruct>
<biblStruct><analytic><author><name sortKey="Chaal, Bk" uniqKey="Chaal B">BK Chaal</name>
</author>
<author><name sortKey="Gupta, Ap" uniqKey="Gupta A">AP Gupta</name>
</author>
<author><name sortKey="Wastuwidyaningtyas, Bd" uniqKey="Wastuwidyaningtyas B">BD Wastuwidyaningtyas</name>
</author>
<author><name sortKey="Luah, Yh" uniqKey="Luah Y">YH Luah</name>
</author>
<author><name sortKey="Bozdech, Z" uniqKey="Bozdech Z">Z Bozdech</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Engel, Ja" uniqKey="Engel J">JA Engel</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Gupta, Ap" uniqKey="Gupta A">AP Gupta</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Ngwa, Cj" uniqKey="Ngwa C">CJ Ngwa</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Trenholme, K" uniqKey="Trenholme K">K Trenholme</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Marfurt, J" uniqKey="Marfurt J">J Marfurt</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Ontoria, Jm" uniqKey="Ontoria J">JM Ontoria</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Hansen, Fk" uniqKey="Hansen F">FK Hansen</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Shen, S" uniqKey="Shen S">S Shen</name>
</author>
<author><name sortKey="Kozikowski, Ap" uniqKey="Kozikowski A">AP Kozikowski</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Van Der Watt, Me" uniqKey="Van Der Watt M">ME van der Watt</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Ngwa, Che Julius" uniqKey="Ngwa C">Che Julius Ngwa</name>
</author>
<author><name sortKey="Kiesow, Meike Jutta" uniqKey="Kiesow M">Meike Jutta Kiesow</name>
</author>
<author><name sortKey="Orchard, Lindsey Marie" uniqKey="Orchard L">Lindsey Marie Orchard</name>
</author>
<author><name sortKey="Farrukh, Afia" uniqKey="Farrukh A">Afia Farrukh</name>
</author>
<author><name sortKey="Llinas, Manuel" uniqKey="Llinas M">Manuel Llinás</name>
</author>
<author><name sortKey="Pradel, Gabriele" uniqKey="Pradel G">Gabriele Pradel</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Ukaegbu, Ue" uniqKey="Ukaegbu U">UE Ukaegbu</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Cui, L" uniqKey="Cui L">L Cui</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Duffy, Mf" uniqKey="Duffy M">MF Duffy</name>
</author>
<author><name sortKey="Selvarajah, Sa" uniqKey="Selvarajah S">SA Selvarajah</name>
</author>
<author><name sortKey="Josling, Ga" uniqKey="Josling G">GA Josling</name>
</author>
<author><name sortKey="Petter, M" uniqKey="Petter M">M Petter</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Merrick, Cj" uniqKey="Merrick C">CJ Merrick</name>
</author>
<author><name sortKey="Duraisingh, Mt" uniqKey="Duraisingh M">MT Duraisingh</name>
</author>
</analytic>
</biblStruct>
<biblStruct></biblStruct>
<biblStruct><analytic><author><name sortKey="Chua, Mj" uniqKey="Chua M">MJ Chua</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Dow, Gs" uniqKey="Dow G">GS Dow</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Giannini, G" uniqKey="Giannini G">G Giannini</name>
</author>
<author><name sortKey="Battistuzzi, G" uniqKey="Battistuzzi G">G Battistuzzi</name>
</author>
<author><name sortKey="Vignola, D" uniqKey="Vignola D">D Vignola</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Sumanadasa, Sd" uniqKey="Sumanadasa S">SD Sumanadasa</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Horrocks, P" uniqKey="Horrocks P">P Horrocks</name>
</author>
<author><name sortKey="Wong, E" uniqKey="Wong E">E Wong</name>
</author>
<author><name sortKey="Russell, K" uniqKey="Russell K">K Russell</name>
</author>
<author><name sortKey="Emes, Rd" uniqKey="Emes R">RD Emes</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Chaal, Bk" uniqKey="Chaal B">BK Chaal</name>
</author>
<author><name sortKey="Gupta, Ap" uniqKey="Gupta A">AP Gupta</name>
</author>
<author><name sortKey="Wastuwidyaningtyas, Bd" uniqKey="Wastuwidyaningtyas B">BD Wastuwidyaningtyas</name>
</author>
<author><name sortKey="Luah, Yh" uniqKey="Luah Y">YH Luah</name>
</author>
<author><name sortKey="Bozdech, Z" uniqKey="Bozdech Z">Z Bozdech</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Hailu, Gs" uniqKey="Hailu G">GS Hailu</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Miranda, Tb" uniqKey="Miranda T">TB Miranda</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Gupta, Ap" uniqKey="Gupta A">AP Gupta</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Karmodiya, K" uniqKey="Karmodiya K">K Karmodiya</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Hoeijmakers, Wa" uniqKey="Hoeijmakers W">WA Hoeijmakers</name>
</author>
<author><name sortKey="Stunnenberg, Hg" uniqKey="Stunnenberg H">HG Stunnenberg</name>
</author>
<author><name sortKey="Bartfai, R" uniqKey="Bartfai R">R Bartfai</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Lai, Ys" uniqKey="Lai Y">YS Lai</name>
</author>
<author><name sortKey="Chen, Jy" uniqKey="Chen J">JY Chen</name>
</author>
<author><name sortKey="Tsai, Hj" uniqKey="Tsai H">HJ Tsai</name>
</author>
<author><name sortKey="Chen, Ty" uniqKey="Chen T">TY Chen</name>
</author>
<author><name sortKey="Hung, Wc" uniqKey="Hung W">WC Hung</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Greiner, D" uniqKey="Greiner D">D Greiner</name>
</author>
<author><name sortKey="Bonaldi, T" uniqKey="Bonaldi T">T Bonaldi</name>
</author>
<author><name sortKey="Eskeland, R" uniqKey="Eskeland R">R Eskeland</name>
</author>
<author><name sortKey="Roemer, E" uniqKey="Roemer E">E Roemer</name>
</author>
<author><name sortKey="Imhof, A" uniqKey="Imhof A">A Imhof</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Eckschlager, Tomas" uniqKey="Eckschlager T">Tomas Eckschlager</name>
</author>
<author><name sortKey="Plch, Johana" uniqKey="Plch J">Johana Plch</name>
</author>
<author><name sortKey="Stiborova, Marie" uniqKey="Stiborova M">Marie Stiborova</name>
</author>
<author><name sortKey="Hrabeta, Jan" uniqKey="Hrabeta J">Jan Hrabeta</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Grozinger, Cm" uniqKey="Grozinger C">CM Grozinger</name>
</author>
<author><name sortKey="Chao, Ed" uniqKey="Chao E">ED Chao</name>
</author>
<author><name sortKey="Blackwell, He" uniqKey="Blackwell H">HE Blackwell</name>
</author>
<author><name sortKey="Moazed, D" uniqKey="Moazed D">D Moazed</name>
</author>
<author><name sortKey="Schreiber, Sl" uniqKey="Schreiber S">SL Schreiber</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Khochbin, S" uniqKey="Khochbin S">S Khochbin</name>
</author>
<author><name sortKey="Verdel, A" uniqKey="Verdel A">A Verdel</name>
</author>
<author><name sortKey="Lemercier, C" uniqKey="Lemercier C">C Lemercier</name>
</author>
<author><name sortKey="Seigneurin Berny, D" uniqKey="Seigneurin Berny D">D Seigneurin-Berny</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Bernstein, Be" uniqKey="Bernstein B">BE Bernstein</name>
</author>
<author><name sortKey="Tong, Jk" uniqKey="Tong J">JK Tong</name>
</author>
<author><name sortKey="Schreiber, Sl" uniqKey="Schreiber S">SL Schreiber</name>
</author>
</analytic>
</biblStruct>
<biblStruct></biblStruct>
<biblStruct><analytic><author><name sortKey="Peck, B" uniqKey="Peck B">B Peck</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Chang, J" uniqKey="Chang J">J Chang</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Finnin, Ms" uniqKey="Finnin M">MS Finnin</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Reader, J" uniqKey="Reader J">J Reader</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Verlinden, Bk" uniqKey="Verlinden B">BK Verlinden</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="D Lessandro, S" uniqKey="D Lessandro S">S D’Alessandro</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Moyo, P" uniqKey="Moyo P">P Moyo</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Ruecker, A" uniqKey="Ruecker A">A Ruecker</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Van Biljon, Ra" uniqKey="Van Biljon R">RA van Biljon</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Hirai, S" uniqKey="Hirai S">S Hirai</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Kikuchi, J" uniqKey="Kikuchi J">J Kikuchi</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Takai, N" uniqKey="Takai N">N Takai</name>
</author>
<author><name sortKey="Narahara, H" uniqKey="Narahara H">H Narahara</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Zappasodi, R" uniqKey="Zappasodi R">R Zappasodi</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Wang, J" uniqKey="Wang J">J Wang</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Janaki Ramaiah, M" uniqKey="Janaki Ramaiah M">M Janaki Ramaiah</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Liao, X" uniqKey="Liao X">X Liao</name>
</author>
</analytic>
</biblStruct>
</listBibl>
</div1>
</back>
</TEI>
<pmc article-type="research-article"><pmc-dir>properties open_access</pmc-dir>
<front><journal-meta><journal-id journal-id-type="nlm-ta">Sci Rep</journal-id>
<journal-id journal-id-type="iso-abbrev">Sci Rep</journal-id>
<journal-title-group><journal-title>Scientific Reports</journal-title>
</journal-title-group>
<issn pub-type="epub">2045-2322</issn>
<publisher><publisher-name>Nature Publishing Group UK</publisher-name>
<publisher-loc>London</publisher-loc>
</publisher>
</journal-meta>
<article-meta><article-id pub-id-type="pmid">32047203</article-id>
<article-id pub-id-type="pmc">7012883</article-id>
<article-id pub-id-type="publisher-id">59298</article-id>
<article-id pub-id-type="doi">10.1038/s41598-020-59298-4</article-id>
<article-categories><subj-group subj-group-type="heading"><subject>Article</subject>
</subj-group>
</article-categories>
<title-group><article-title>Epigenetic inhibitors target multiple stages of <italic>Plasmodium falciparum</italic>
parasites</article-title>
</title-group>
<contrib-group><contrib contrib-type="author" equal-contrib="yes"><name><surname>Coetzee</surname>
<given-names>Nanika</given-names>
</name>
<xref ref-type="aff" rid="Aff1"></xref>
</contrib>
<contrib contrib-type="author" equal-contrib="yes"><name><surname>von Grüning</surname>
<given-names>Hilde</given-names>
</name>
<xref ref-type="aff" rid="Aff1"></xref>
</contrib>
<contrib contrib-type="author"><name><surname>Opperman</surname>
<given-names>Daniel</given-names>
</name>
<xref ref-type="aff" rid="Aff1"></xref>
</contrib>
<contrib contrib-type="author"><name><surname>van der Watt</surname>
<given-names>Mariette</given-names>
</name>
<xref ref-type="aff" rid="Aff1"></xref>
</contrib>
<contrib contrib-type="author"><name><surname>Reader</surname>
<given-names>Janette</given-names>
</name>
<xref ref-type="aff" rid="Aff1"></xref>
</contrib>
<contrib contrib-type="author" corresp="yes"><name><surname>Birkholtz</surname>
<given-names>Lyn-Marié</given-names>
</name>
<address><email>lbirkholtz@up.ac.za</email>
</address>
<xref ref-type="aff" rid="Aff1"></xref>
</contrib>
<aff id="Aff1"><institution-wrap><institution-id institution-id-type="ISNI">0000 0001 2107 2298</institution-id>
<institution-id institution-id-type="GRID">grid.49697.35</institution-id>
<institution>Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control,</institution>
<institution>University of Pretoria,</institution>
</institution-wrap>
Private Bag x20, Hatfield, 0028 South Africa</aff>
</contrib-group>
<pub-date pub-type="epub"><day>11</day>
<month>2</month>
<year>2020</year>
</pub-date>
<pub-date pub-type="pmc-release"><day>11</day>
<month>2</month>
<year>2020</year>
</pub-date>
<pub-date pub-type="collection"><year>2020</year>
</pub-date>
<volume>10</volume>
<elocation-id>2355</elocation-id>
<history><date date-type="received"><day>8</day>
<month>11</month>
<year>2019</year>
</date>
<date date-type="accepted"><day>16</day>
<month>12</month>
<year>2019</year>
</date>
</history>
<permissions><copyright-statement>© The Author(s) 2020</copyright-statement>
<license license-type="OpenAccess"><license-p><bold>Open Access</bold>
This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit <ext-link ext-link-type="uri" xlink:href="http://creativecommons.org/licenses/by/4.0/">http://creativecommons.org/licenses/by/4.0/</ext-link>
.</license-p>
</license>
</permissions>
<abstract id="Abs1"><p id="Par1">The epigenome of the malaria parasite, <italic>Plasmodium falciparum</italic>
, is associated with regulation of various essential processes in the parasite including control of proliferation during asexual development as well as control of sexual differentiation. The unusual nature of the epigenome has prompted investigations into the potential to target epigenetic modulators with novel chemotypes. Here, we explored the diversity within a library of 95 compounds, active against various epigenetic modifiers in cancerous cells, for activity against multiple stages of <italic>P. falciparum</italic>
development. We show that <italic>P. falciparum</italic>
is differentially susceptible to epigenetic perturbation during both asexual and sexual development, with early stage gametocytes particularly sensitive to epi-drugs targeting both histone and non-histone epigenetic modifiers. Moreover, 5 compounds targeting histone acetylation and methylation show potent multistage activity against asexual parasites, early and late stage gametocytes, with transmission-blocking potential. Overall, these results warrant further examination of the potential antimalarial properties of these hit compounds.</p>
</abstract>
<kwd-group kwd-group-type="npg-subject"><title>Subject terms</title>
<kwd>Drug discovery</kwd>
<kwd>Diseases</kwd>
</kwd-group>
<custom-meta-group><custom-meta><meta-name>issue-copyright-statement</meta-name>
<meta-value>© The Author(s) 2020</meta-value>
</custom-meta>
</custom-meta-group>
</article-meta>
</front>
</pmc>
<affiliations><list></list>
<tree><noCountry><name sortKey="Birkholtz, Lyn Marie" sort="Birkholtz, Lyn Marie" uniqKey="Birkholtz L" first="Lyn-Marié" last="Birkholtz">Lyn-Marié Birkholtz</name>
<name sortKey="Coetzee, Nanika" sort="Coetzee, Nanika" uniqKey="Coetzee N" first="Nanika" last="Coetzee">Nanika Coetzee</name>
<name sortKey="Opperman, Daniel" sort="Opperman, Daniel" uniqKey="Opperman D" first="Daniel" last="Opperman">Daniel Opperman</name>
<name sortKey="Reader, Janette" sort="Reader, Janette" uniqKey="Reader J" first="Janette" last="Reader">Janette Reader</name>
<name sortKey="Van Der Watt, Mariette" sort="Van Der Watt, Mariette" uniqKey="Van Der Watt M" first="Mariette" last="Van Der Watt">Mariette Van Der Watt</name>
<name sortKey="Von Gruning, Hilde" sort="Von Gruning, Hilde" uniqKey="Von Gruning H" first="Hilde" last="Von Grüning">Hilde Von Grüning</name>
</noCountry>
</tree>
</affiliations>
</record>
Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/ChloroquineV1/Data/Pmc/Checkpoint
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000150 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Pmc/Checkpoint/biblio.hfd -nk 000150 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien |wiki= Sante |area= ChloroquineV1 |flux= Pmc |étape= Checkpoint |type= RBID |clé= PMC:7012883 |texte= Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites }}
Pour générer des pages wiki
HfdIndexSelect -h $EXPLOR_AREA/Data/Pmc/Checkpoint/RBID.i -Sk "pubmed:32047203" \ | HfdSelect -Kh $EXPLOR_AREA/Data/Pmc/Checkpoint/biblio.hfd \ | NlmPubMed2Wicri -a ChloroquineV1
![]() | This area was generated with Dilib version V0.6.33. | ![]() |