Literature DB >> 32366713

Activity of Epigenetic Inhibitors against Plasmodium falciparum Asexual and Sexual Blood Stages.

Leen N Vanheer1, Hao Zhang1, Gang Lin1, Björn F C Kafsack2.   

Abstract

Earlier genetic and inhibitor studies showed that epigenetic regulation of gene expression is critical for malaria parasite survival in multiple life stages and a promising target for new antimalarials. We therefore evaluated the activity of 350 diverse epigenetic inhibitors against multiple stages of Plasmodium falciparum We observed ≥90% inhibition at 10 μM for 28% of compounds against asexual blood stages and early gametocytes, of which a third retained ≥90% inhibition at 1 μM.
Copyright © 2020 American Society for Microbiology.

Entities:  

Keywords:  Plasmodium falciparum; antimalarial agents; drug screening; epigenetic inhibitors; malaria; small-molecule screen

Mesh:

Substances:

Year:  2020        PMID: 32366713      PMCID: PMC7318029          DOI: 10.1128/AAC.02523-19

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  28 in total

1.  Heterochromatin protein 1 secures survival and transmission of malaria parasites.

Authors:  Nicolas M B Brancucci; Nicole L Bertschi; Lei Zhu; Igor Niederwieser; Wai Hoe Chin; Rahel Wampfler; Céline Freymond; Matthias Rottmann; Ingrid Felger; Zbynek Bozdech; Till S Voss
Journal:  Cell Host Microbe       Date:  2014-08-13       Impact factor: 21.023

2.  A Plasmodium falciparum histone deacetylase regulates antigenic variation and gametocyte conversion.

Authors:  Bradley I Coleman; Kristen M Skillman; Rays H Y Jiang; Lauren M Childs; Lindsey M Altenhofen; Markus Ganter; Yvette Leung; Ilana Goldowitz; Björn F C Kafsack; Matthias Marti; Manuel Llinás; Caroline O Buckee; Manoj T Duraisingh
Journal:  Cell Host Microbe       Date:  2014-08-13       Impact factor: 21.023

3.  Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.

Authors:  Finn K Hansen; Subathdrage D M Sumanadasa; Katharina Stenzel; Sandra Duffy; Stephan Meister; Linda Marek; Rebekka Schmetter; Krystina Kuna; Alexandra Hamacher; Benjamin Mordmüller; Matthias U Kassack; Elizabeth A Winzeler; Vicky M Avery; Katherine T Andrews; Thomas Kurz
Journal:  Eur J Med Chem       Date:  2014-05-22       Impact factor: 6.514

Review 4.  HDAC inhibitors in parasitic diseases.

Authors:  Katherine T Andrews; Ashraful Haque; Malcolm K Jones
Journal:  Immunol Cell Biol       Date:  2011-11-29       Impact factor: 5.126

5.  Identification of novel quinazoline derivatives as potent antiplasmodial agents.

Authors:  Anne Bouchut; Dante Rotili; Christine Pierrot; Sergio Valente; Sophia Lafitte; Johan Schultz; Urban Hoglund; Roberta Mazzone; Alessia Lucidi; Giancarlo Fabrizi; Dany Pechalrieu; Paola B Arimondo; Tina S Skinner-Adams; Ming Jang Chua; Kathy T Andrews; Antonello Mai; Jamal Khalife
Journal:  Eur J Med Chem       Date:  2018-10-17       Impact factor: 6.514

6.  A Unique Virulence Gene Occupies a Principal Position in Immune Evasion by the Malaria Parasite Plasmodium falciparum.

Authors:  Uchechi E Ukaegbu; Xu Zhang; Adina R Heinberg; Mamadou Wele; Qijun Chen; Kirk W Deitsch
Journal:  PLoS Genet       Date:  2015-05-19       Impact factor: 5.917

7.  Transcriptional Profiling Defines Histone Acetylation as a Regulator of Gene Expression during Human-to-Mosquito Transmission of the Malaria Parasite Plasmodium falciparum.

Authors:  Che J Ngwa; Meike J Kiesow; Olga Papst; Lindsey M Orchard; Michael Filarsky; Alina N Rosinski; Till S Voss; Manuel Llinás; Gabriele Pradel
Journal:  Front Cell Infect Microbiol       Date:  2017-07-24       Impact factor: 5.293

8.  Comparative Heterochromatin Profiling Reveals Conserved and Unique Epigenome Signatures Linked to Adaptation and Development of Malaria Parasites.

Authors:  Sabine A Fraschka; Michael Filarsky; Regina Hoo; Igor Niederwieser; Xue Yan Yam; Nicolas M B Brancucci; Franziska Mohring; Annals T Mushunje; Ximei Huang; Peter R Christensen; Francois Nosten; Zbynek Bozdech; Bruce Russell; Robert W Moon; Matthias Marti; Peter R Preiser; Richárd Bártfai; Till S Voss
Journal:  Cell Host Microbe       Date:  2018-03-01       Impact factor: 21.023

9.  The G9a Histone Methyltransferase Inhibitor BIX-01294 Modulates Gene Expression during Plasmodium falciparum Gametocyte Development and Transmission.

Authors:  Che Julius Ngwa; Meike Jutta Kiesow; Lindsey Marie Orchard; Afia Farrukh; Manuel Llinás; Gabriele Pradel
Journal:  Int J Mol Sci       Date:  2019-10-14       Impact factor: 5.923

10.  Changes in genome organization of parasite-specific gene families during the Plasmodium transmission stages.

Authors:  Evelien M Bunnik; Kate B Cook; Nelle Varoquaux; Gayani Batugedara; Jacques Prudhomme; Anthony Cort; Lirong Shi; Chiara Andolina; Leila S Ross; Declan Brady; David A Fidock; Francois Nosten; Rita Tewari; Photini Sinnis; Ferhat Ay; Jean-Philippe Vert; William Stafford Noble; Karine G Le Roch
Journal:  Nat Commun       Date:  2018-05-15       Impact factor: 14.919

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  7 in total

1.  Activity Comparison of Epigenetic Modulators against the Hemoprotozoan Parasites Babesia divergens and Plasmodium falciparum.

Authors:  Leen N Vanheer; Björn F C Kafsack
Journal:  ACS Infect Dis       Date:  2021-02-18       Impact factor: 5.578

2.  A novel multistage antiplasmodial inhibitor targeting Plasmodium falciparum histone deacetylase 1.

Authors:  Zhenghui Huang; Ruoxi Li; Tongke Tang; Dazheng Ling; Manjiong Wang; Dandan Xu; Maoxin Sun; Lulu Zheng; Feng Zhu; Hui Min; Rachasak Boonhok; Yan Ding; Yuhao Wen; Yicong Chen; Xiaokang Li; Yuxi Chen; Taiping Liu; Jiping Han; Jun Miao; Qiang Fang; Yaming Cao; Yun Tang; Jie Cui; Wenyue Xu; Liwang Cui; Jin Zhu; Gary Wong; Jian Li; Lubin Jiang
Journal:  Cell Discov       Date:  2020-12-11       Impact factor: 10.849

Review 3.  "Reading" a new chapter in protozoan parasite transcriptional regulation.

Authors:  Krista Fleck; Malorie Nitz; Victoria Jeffers
Journal:  PLoS Pathog       Date:  2021-12-02       Impact factor: 6.823

4.  Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183.

Authors:  Taco W A Kooij; Koen J Dechering; Laura E de Vries; Patrick A M Jansen; Catalina Barcelo; Justin Munro; Julie M J Verhoef; Charisse Flerida A Pasaje; Kelly Rubiano; Josefine Striepen; Nada Abla; Luuk Berning; Judith M Bolscher; Claudia Demarta-Gatsi; Rob W M Henderson; Tonnie Huijs; Karin M J Koolen; Patrick K Tumwebaze; Tomas Yeo; Anna C C Aguiar; Iñigo Angulo-Barturen; Alisje Churchyard; Jake Baum; Benigno Crespo Fernández; Aline Fuchs; Francisco-Javier Gamo; Rafael V C Guido; María Belén Jiménez-Diaz; Dhelio B Pereira; Rosemary Rochford; Camille Roesch; Laura M Sanz; Graham Trevitt; Benoit Witkowski; Sergio Wittlin; Roland A Cooper; Philip J Rosenthal; Robert W Sauerwein; Joost Schalkwijk; Pedro H H Hermkens; Roger V Bonnert; Brice Campo; David A Fidock; Manuel Llinás; Jacquin C Niles
Journal:  Nat Commun       Date:  2022-04-20       Impact factor: 17.694

Review 5.  Adapt or Die: Targeting Unique Transmission-Stage Biology for Malaria Elimination.

Authors:  Mariëtte E van der Watt; Janette Reader; Lyn-Marié Birkholtz
Journal:  Front Cell Infect Microbiol       Date:  2022-06-09       Impact factor: 6.073

6.  H3K36 methylation reprograms gene expression to drive early gametocyte development in Plasmodium falciparum.

Authors:  Jessica Connacher; Gabrielle A Josling; Lindsey M Orchard; Janette Reader; Manuel Llinás; Lyn-Marié Birkholtz
Journal:  Epigenetics Chromatin       Date:  2021-04-01       Impact factor: 4.954

7.  Beyond phosphorylation: Putative roles of post-translational modifications in Plasmodium sexual stages.

Authors:  Nila Johnson; Nisha Philip
Journal:  Mol Biochem Parasitol       Date:  2021-07-27       Impact factor: 1.759

  7 in total

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