Imperial College London
Portrait Picture

Prof Ed Tate

Faculty of Natural Sciences, Department of Chemistry

GSK Chair in Chemical Biology
 
 
 
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Contact

 

+44 (0)20 7594 3752e.tate Website CV

 
 
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Assistant

 

Ms Agnes Lee +44 (0)20 7594 9852

 
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Location

 

301BMolecular Sciences Research HubWhite City Campus

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Summary

 

Publications

Citation

BibTex format

@article{Hong:2019:10.1073/pnas.1816585116,
author = {Hong, WD and Benayoud, F and Nixon, GL and Ford, L and Johnston, KL and Clare, RH and Cassidy, A and Cook, DAN and Siu, A and Shiotani, M and Webborn, PJH and Kavanagh, S and Aljayyoussi, G and Murphy, E and Steven, A and Archer, J and Struever, D and Frohberger, SJ and Ehrens, A and Huebner, MP and Hoerauf, A and Roberts, AP and Hubbard, ATM and Tate, EW and Serwa, RA and Leung, SC and Qie, L and Berry, NG and Gusovsky, F and Hemingway, J and Turner, JD and Taylor, MJ and Ward, SA and O'Neill, PM},
doi = {10.1073/pnas.1816585116},
journal = {Proceedings of the National Academy of Sciences of the United States of America},
pages = {1414--1419},
title = {AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis},
url = {http://dx.doi.org/10.1073/pnas.1816585116},
volume = {116},
year = {2019}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - Onchocerciasis and lymphatic filariasis are two neglected tropical diseases that together affect ∼157 million people and inflict severe disability. Both diseases are caused by parasitic filarial nematodes with elimination efforts constrained by the lack of a safe drug that can kill the adult filaria (macrofilaricide). Previous proof-of-concept human trials have demonstrated that depleting >90% of the essential nematode endosymbiont bacterium, Wolbachia, using antibiotics, can lead to permanent sterilization of adult female parasites and a safe macrofilaricidal outcome. AWZ1066S is a highly specific anti-Wolbachia candidate selected through a lead optimization program focused on balancing efficacy, safety and drug metabolism/pharmacokinetic (DMPK) features of a thienopyrimidine/quinazoline scaffold derived from phenotypic screening. AWZ1066S shows superior efficacy to existing anti-Wolbachia therapies in validated preclinical models of infection and has DMPK characteristics that are compatible with a short therapeutic regimen of 7 days or less. This candidate molecule is well-positioned for onward development and has the potential to make a significant impact on communities affected by filariasis.
AU  - Hong,WD
AU  - Benayoud,F
AU  - Nixon,GL
AU  - Ford,L
AU  - Johnston,KL
AU  - Clare,RH
AU  - Cassidy,A
AU  - Cook,DAN
AU  - Siu,A
AU  - Shiotani,M
AU  - Webborn,PJH
AU  - Kavanagh,S
AU  - Aljayyoussi,G
AU  - Murphy,E
AU  - Steven,A
AU  - Archer,J
AU  - Struever,D
AU  - Frohberger,SJ
AU  - Ehrens,A
AU  - Huebner,MP
AU  - Hoerauf,A
AU  - Roberts,AP
AU  - Hubbard,ATM
AU  - Tate,EW
AU  - Serwa,RA
AU  - Leung,SC
AU  - Qie,L
AU  - Berry,NG
AU  - Gusovsky,F
AU  - Hemingway,J
AU  - Turner,JD
AU  - Taylor,MJ
AU  - Ward,SA
AU  - O'Neill,PM
DO  - 10.1073/pnas.1816585116
EP  - 1419
PY  - 2019///
SN  - 0027-8424
SP  - 1414
TI  - AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis
T2  - Proceedings of the National Academy of Sciences of the United States of America
UR  - http://dx.doi.org/10.1073/pnas.1816585116
UR  - http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000456336100049&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
UR  - http://hdl.handle.net/10044/1/67498
VL  - 116
ER  -
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