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Citation

BibTex format

@article{Lubin:2018:10.1021/acsinfecdis.7b00228,
author = {Lubin, AS and Zubiaurre, AR and Matthews, H and Baumann, H and Fisher, FR and Morales-Sanfrutos, J and Hadavizadeh, KS and Nardella, F and Tate, EW and Baum, J and Scherf, A and Fuchter, MJ},
doi = {10.1021/acsinfecdis.7b00228},
journal = {ACS Infectious Diseases},
pages = {523--530},
title = {Development of a photo-crosslinkable diaminoquinazoline inhibitor for target identification in plasmodium falciparum},
url = {http://dx.doi.org/10.1021/acsinfecdis.7b00228},
volume = {4},
year = {2018}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - Diaminoquinazolines represent a privileged scaffold for antimalarial discovery, including use as putative Plasmodium histone lysine methyltransferase inhibitors. Despite this, robust evidence for their molecular targets is lacking. Here we report the design and development of a small-molecule photo-crosslinkable probe to investigate the targets of our diaminoquinazoline series. We demonstrate the effectiveness of our designed probe for photoaffinity labelling of Plasmodium lysates and identify similarities between the target profiles of the probe and the representative diaminoquinazoline BIX-01294. Initial pull-down proteomics experiments identified 104 proteins from different classes, many of which are essential, highlighting the suitability of the developed probe as a valuable tool for target identification in Plasmodium falciparum.
AU  - Lubin,AS
AU  - Zubiaurre,AR
AU  - Matthews,H
AU  - Baumann,H
AU  - Fisher,FR
AU  - Morales-Sanfrutos,J
AU  - Hadavizadeh,KS
AU  - Nardella,F
AU  - Tate,EW
AU  - Baum,J
AU  - Scherf,A
AU  - Fuchter,MJ
DO  - 10.1021/acsinfecdis.7b00228
EP  - 530
PY  - 2018///
SN  - 2373-8227
SP  - 523
TI  - Development of a photo-crosslinkable diaminoquinazoline inhibitor for target identification in plasmodium falciparum
T2  - ACS Infectious Diseases
UR  - http://dx.doi.org/10.1021/acsinfecdis.7b00228
UR  - http://hdl.handle.net/10044/1/56772
VL  - 4
ER  -
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Contact

Prof. Ed Tate
GSK Chair in Chemical Biology
Department of Chemistry
Molecular Sciences Research Hub, White City Campus,
82 Wood Lane, London, W12 0BZ

e.tate@imperial.ac.uk
Tel: +44 (0)20 759 + ext 43752 or 45821