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| Content Provider | PubMed Central |
|---|---|
| Author | Beatriz, Baragaña 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 Achim, Porzelle Martínez, María Santos Bolscher, Judith M. Woodland, Andrew Norval, Suzanne Fabio, Zuccotto Thomas, John Simeons, Frederick Stojanovski, Laste Maria, Osuna-cabello Brock, Paddy M. Churcher, Tom S. Sala, Katarzyna A. Zakutansky, Sara E. Belén, Jiménez-díaz María Sanz, Laura Maria Riley, Jennifer Basak, Rajshekhar Campbell, Michael Avery, Vicky M. Sauerwein, Robert W. Dechering, Koen J. Noviyanti, Rintis Campo, Brice Frearson, Julie A. Iñigo, Angulo-barturen Santiago, Ferrer-bazaga Gamo, Francisco Javier Wyatt, Paul G. Leroy, Didier Siegl, Peter Delves, Michael J. Kyle, Dennis E. Wittlin, Sergio Marfurt, Jutta Price, Ric N. Sinden, Robert E. Winzeler, Elizabeth Charman, Susan A. Bebrevska, Lidiya Gray, David W. Campbell, Simon Fairlamb, Alan H. Willis, Paul Rayner, Julian C. Fidock, David A. Read, Kevin D. Gilbert, Ian H. |
| 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. We describe the discovery of DDD107498, a compound with a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the 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 mRNA, and is essential for protein synthesis. This discovery of eEF2 as a viable antimalarial drug target opens up new possibilities for drug discovery. |
| Related Links | http://dx.doi.org/10.1038/nature14451 |
| Starting Page | 315 |
| File Format | |
| ISSN | 14764687 |
| e-ISSN | 14764687 |
| Journal | Nature |
| Issue Number | 7556 |
| Volume Number | 522 |
| Language | English |
| Publisher Date | 2015-06-18 |
| Access Restriction | Open |
| Subject Keyword | Research in Higher Education |
| Content Type | Text |
| Resource Type | Article |
| Subject | Multidisciplinary |
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