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A novel multiple-stage antimalarial agent that inhibits protein synthesis

Baragan, Beatriz, Hallyburton, Irene, Lee, Marcus C. S., Norcross, Neil R., Grimaldi, Raffaella, Otto, Thomas D., Proto, William R., Blagborough, Andrew M., Meister, Stephan, Wirjanata, Grennady, Ruecker, Andrea, Upton, Leanna M., Abraham, Tara S., Almeida, Mariana J., Pradhan, Anupam, Porzelle, Achim, Martinez, Maria S., Bolscher, Judith M., Marfurt, Jutta, Price, Ric N. and et al. (2015). A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature,522(7556):315-320.

Document type: Journal Article
Citation counts: Altmetric Score Altmetric Score is 384
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IRMA ID 11381xPUB135
Title A novel multiple-stage antimalarial agent that inhibits protein synthesis
Author Baragan, Beatriz
Hallyburton, Irene
Lee, Marcus C. S.
Norcross, Neil R.
Grimaldi, Raffaella
Otto, Thomas D.
Proto, William R.
Blagborough, Andrew M.
Meister, Stephan
Wirjanata, Grennady
Ruecker, Andrea
Upton, Leanna M.
Abraham, Tara S.
Almeida, Mariana J.
Pradhan, Anupam
Porzelle, Achim
Martinez, Maria S.
Bolscher, Judith M.
Marfurt, Jutta
Price, Ric N.
et al.
Journal Name Nature
Publication Date 2015
Volume Number 522
Issue Number 7556
ISSN 0028-0836   (check CDU catalogue open catalogue search in new window)
Scopus ID 2-s2.0-84934976258
Start Page 315
End Page 320
Total Pages 6
Place of Publication United Kingdom
Publisher Nature Publishing Group
Field of Research MEDICAL AND HEALTH SCIENCES
HERDC Category C1 - Journal Article (DIISR)
Abstract There is an urgent need for new drugs to treat malaria, with broad therapeutic potential and novel modes of action, to widen the scope of treatment and to overcome emerging drug resistance. Here we describe the discovery of DDD107498, a compound with a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the Plasmodium parasite, with good pharmacokinetic properties and an acceptable safety profile. DDD107498 demonstrates potential to address a variety of clinical needs, including single-dose treatment, transmission blocking and chemoprotection. DDD107498 was developed from a screening programme against blood-stage malaria parasites; its molecular target has been identified as translation elongation factor 2 (eEF2), which is responsible for the GTP-dependent translocation of the ribosome along messenger RNA, and is essential for protein synthesis. This discovery of eEF2 as a viable antimalarial drug target opens up new possibilities for drug discovery.
Keywords Drug discovery and development
Target identification
Malaria
DOI http://dx.doi.org/10.1038/nature14451   (check subscription with CDU E-Gateway service for CDU Staff and Students  check subscription with CDU E-Gateway in new window)
 
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