Imperial College London
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Professor Jake Baum

Faculty of Natural Sciences, Department of Life Sciences

Visiting Professor
 
 
 
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Contact

 

+44 (0)20 7594 5420jake.baum Website

 
 
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Location

 

c/o Baum labSir Alexander Fleming BuildingSouth Kensington Campus

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Summary

 

Publications

Citation

BibTex format

@article{Miguel-Blanco:2017:10.1038/ncomms15160,
author = {Miguel-Blanco, C and Molina, I and Bardera, AI and Diaz, B and de, las Heras L and Lozano, S and Gonzalez, C and Rodrigues, J and Delves, MJ and Ruecker, A and Colmenarejo, G and Viera, S and Martinez-Martinez, MS and Fernandez, E and Baum, J and Sinden, RE and Herreros, E},
doi = {10.1038/ncomms15160},
journal = {Nature Communications},
title = {Hundreds of dual-stage antimalarial molecules discovered by a functional gametocyte screen},
url = {http://dx.doi.org/10.1038/ncomms15160},
volume = {8},
year = {2017}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - Plasmodium falciparum stage V gametocytes are responsible for parasite transmission, and drugs targeting this stage are needed to support malaria elimination. We here screen the Tres Cantos Antimalarial Set (TCAMS) using the previously developed P. falciparum female gametocyte activation assay (Pf FGAA), which assesses stage V female gametocyte viability and functionality using Pfs25 expression. We identify over 400 compounds with activities <2 μM, chemically classified into 57 clusters and 33 singletons. Up to 68% of the hits are chemotypes described for the first time as late-stage gametocyte-targeting molecules. In addition, the biological profile of 90 compounds representing the chemical diversity is assessed. We confirm in vitro transmission-blocking activity of four of the six selected molecules belonging to three distinct scaffold clusters. Overall, this TCAMS gametocyte screen provides 276 promising antimalarial molecules with dual asexual/sexual activity, representing starting points for target identification and candidate selection.
AU  - Miguel-Blanco,C
AU  - Molina,I
AU  - Bardera,AI
AU  - Diaz,B
AU  - de,las Heras L
AU  - Lozano,S
AU  - Gonzalez,C
AU  - Rodrigues,J
AU  - Delves,MJ
AU  - Ruecker,A
AU  - Colmenarejo,G
AU  - Viera,S
AU  - Martinez-Martinez,MS
AU  - Fernandez,E
AU  - Baum,J
AU  - Sinden,RE
AU  - Herreros,E
DO  - 10.1038/ncomms15160
PY  - 2017///
SN  - 2041-1723
TI  - Hundreds of dual-stage antimalarial molecules discovered by a functional gametocyte screen
T2  - Nature Communications
UR  - http://dx.doi.org/10.1038/ncomms15160
UR  - http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000401508900001&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
UR  - http://hdl.handle.net/10044/1/49100
VL  - 8
ER  -
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