Imperial College London
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Professor Matthew J. Fuchter

Faculty of Natural Sciences, Department of Chemistry

Professor of Chemistry
 
 
 
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Contact

 

+44 (0)20 7594 5815m.fuchter

 
 
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Location

 

110DMolecular Sciences Research HubWhite City Campus

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Summary

 

Publications

Citation

BibTex format

@article{Miguel-Blanco:2021:10.1038/s41598-021-81343-z,
author = {Miguel-Blanco, C and Murithi, JM and Benavente, ED and Angrisano, F and Sala, KA and van, Schalkwyk DA and Vanaerschot, M and Schwach, F and Fuchter, MJ and Billker, O and Sutherland, CJ and Campino, SG and Clark, TG and Blagborough, AM and Fidock, DA and Herreros, E and Gamo, FJ and Baum, J and Delves, MJ},
doi = {10.1038/s41598-021-81343-z},
journal = {Scientific Reports},
title = {The antimalarial efficacy and mechanism of resistance of the novel chemotype DDD01034957},
url = {http://dx.doi.org/10.1038/s41598-021-81343-z},
volume = {11},
year = {2021}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - New antimalarial therapeutics are needed to ensure that malaria cases continue to be driven down, as both emerging parasite resistance to frontline chemotherapies and mosquito resistance to current insecticides threaten control programmes. Plasmodium, the apicomplexan parasite responsible for malaria, causes disease pathology through repeated cycles of invasion and replication within host erythrocytes (the asexual cycle). Antimalarial drugs primarily target this cycle, seeking to reduce parasite burden within the host as fast as possible and to supress recrudescence for as long as possible. Intense phenotypic drug screening efforts have identified a number of promising new antimalarial molecules. Particularly important is the identification of compounds with new modes of action within the parasite to combat existing drug resistance and suitable for formulation of efficacious combination therapies. Here we detail the antimalarial properties of DDD01034957-a novel antimalarial molecule which is fast-acting and potent against drug resistant strains in vitro, shows activity in vivo, and possesses a resistance mechanism linked to the membrane transporter PfABCI3. These data support further medicinal chemistry lead-optimization of DDD01034957 as a novel antimalarial chemical class and provide new insights to further reduce in vivo metabolic clearance.
AU  - Miguel-Blanco,C
AU  - Murithi,JM
AU  - Benavente,ED
AU  - Angrisano,F
AU  - Sala,KA
AU  - van,Schalkwyk DA
AU  - Vanaerschot,M
AU  - Schwach,F
AU  - Fuchter,MJ
AU  - Billker,O
AU  - Sutherland,CJ
AU  - Campino,SG
AU  - Clark,TG
AU  - Blagborough,AM
AU  - Fidock,DA
AU  - Herreros,E
AU  - Gamo,FJ
AU  - Baum,J
AU  - Delves,MJ
DO  - 10.1038/s41598-021-81343-z
PY  - 2021///
SN  - 2045-2322
TI  - The antimalarial efficacy and mechanism of resistance of the novel chemotype DDD01034957
T2  - Scientific Reports
UR  - http://dx.doi.org/10.1038/s41598-021-81343-z
UR  - https://www.ncbi.nlm.nih.gov/pubmed/33479319
UR  - http://hdl.handle.net/10044/1/86336
VL  - 11
ER  -
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