BibTex format
@article{Baragana:2015:10.1038/nature14451,
author = {Baragana, B and Hallyburton, I and Lee, MCS and Norcross, NR and Grimaldi, R and Otto, TD and Proto, WR and Blagborough, AM and Meister, S and Wirjanata, G and Ruecker, A and Upton, LM and Abraham, TS and Almeida, MJ and Pradhan, A and Porzelle, A and Santos, Martinez M and Bolscher, JM and Woodland, A and Norval, S and Zuccotto, F and Thomas, J and Simeons, F and Stojanovski, L and Osuna-Cabello, M and Brock, PM and Churcher, TS and Sala, KA and Zakutansky, SE and Belen, Jimenez-Diaz M and Maria, Sanz L and Riley, J and Basak, R and Campbell, M and Avery, VM and Sauerwein, RW and Dechering, KJ and Noviyanti, R and Campo, B and Frearson, JA and Angulo-Barturen, I and Ferrer-Bazaga, S and Javier, Gamo F and Wyatt, PG and Leroy, D and Siegl, P and Delves, MJ and Kyle, DE and Wittlin, S and Marfurt, J and Price, RN and Sinden, RE and Winzeler, EA and Charman, SA and Bebrevska, L and Gray, DW and Campbell, S and Fairlamb, AH and Willis, PA and Rayner, JC and Fidock, DA and Read, KD and Gil},
doi = {10.1038/nature14451},
journal = {Nature},
pages = {315--320},
title = {A novel multiple-stage antimalarial agent that inhibits protein synthesis},
url = {http://dx.doi.org/10.1038/nature14451},
volume = {522},
year = {2015}
}
RIS format (EndNote, RefMan)
TY - JOUR
AB - 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.
AU - Baragana,B
AU - Hallyburton,I
AU - Lee,MCS
AU - Norcross,NR
AU - Grimaldi,R
AU - Otto,TD
AU - Proto,WR
AU - Blagborough,AM
AU - Meister,S
AU - Wirjanata,G
AU - Ruecker,A
AU - Upton,LM
AU - Abraham,TS
AU - Almeida,MJ
AU - Pradhan,A
AU - Porzelle,A
AU - Santos,Martinez M
AU - Bolscher,JM
AU - Woodland,A
AU - Norval,S
AU - Zuccotto,F
AU - Thomas,J
AU - Simeons,F
AU - Stojanovski,L
AU - Osuna-Cabello,M
AU - Brock,PM
AU - Churcher,TS
AU - Sala,KA
AU - Zakutansky,SE
AU - Belen,Jimenez-Diaz M
AU - Maria,Sanz L
AU - Riley,J
AU - Basak,R
AU - Campbell,M
AU - Avery,VM
AU - Sauerwein,RW
AU - Dechering,KJ
AU - Noviyanti,R
AU - Campo,B
AU - Frearson,JA
AU - Angulo-Barturen,I
AU - Ferrer-Bazaga,S
AU - Javier,Gamo F
AU - Wyatt,PG
AU - Leroy,D
AU - Siegl,P
AU - Delves,MJ
AU - Kyle,DE
AU - Wittlin,S
AU - Marfurt,J
AU - Price,RN
AU - Sinden,RE
AU - Winzeler,EA
AU - Charman,SA
AU - Bebrevska,L
AU - Gray,DW
AU - Campbell,S
AU - Fairlamb,AH
AU - Willis,PA
AU - Rayner,JC
AU - Fidock,DA
AU - Read,KD
AU - Gilbert,IH
DO - 10.1038/nature14451
EP - 320
PY - 2015///
SN - 0028-0836
SP - 315
TI - A novel multiple-stage antimalarial agent that inhibits protein synthesis
T2 - Nature
UR - http://dx.doi.org/10.1038/nature14451
VL - 522
ER -