Fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice

Glycolytic enzymes are challenging drug targets due to their highly conserved active sites and phosphorylated substrates. Here, the authors identify fast acting allosteric inhibitors of Trypanosoma brucei phosphofructokinase that block trypanosome glycolysis and provide cure evidence in murine model...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Iain W. McNae, James Kinkead, Divya Malik, Li-Hsuan Yen, Martin K. Walker, Chris Swain, Scott P. Webster, Nick Gray, Peter M. Fernandes, Elmarie Myburgh, Elizabeth A. Blackburn, Ryan Ritchie, Carol Austin, Martin A. Wear, Adrian J. Highton, Andrew J. Keats, Antonio Vong, Jacqueline Dornan, Jeremy C. Mottram, Paul A. M. Michels, Simon Pettit, Malcolm D. Walkinshaw
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/4b5f2d939f554cc8b893fd1148232b4e
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:4b5f2d939f554cc8b893fd1148232b4e
record_format	dspace
spelling	oai:doaj.org-article:4b5f2d939f554cc8b893fd1148232b4e2021-12-02T12:11:11ZFast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice10.1038/s41467-021-21273-62041-1723https://doaj.org/article/4b5f2d939f554cc8b893fd1148232b4e2021-02-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-21273-6https://doaj.org/toc/2041-1723Glycolytic enzymes are challenging drug targets due to their highly conserved active sites and phosphorylated substrates. Here, the authors identify fast acting allosteric inhibitors of Trypanosoma brucei phosphofructokinase that block trypanosome glycolysis and provide cure evidence in murine model.Iain W. McNaeJames KinkeadDivya MalikLi-Hsuan YenMartin K. WalkerChris SwainScott P. WebsterNick GrayPeter M. FernandesElmarie MyburghElizabeth A. BlackburnRyan RitchieCarol AustinMartin A. WearAdrian J. HightonAndrew J. KeatsAntonio VongJacqueline DornanJeremy C. MottramPaul A. M. MichelsSimon PettitMalcolm D. WalkinshawNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-10 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Iain W. McNae James Kinkead Divya Malik Li-Hsuan Yen Martin K. Walker Chris Swain Scott P. Webster Nick Gray Peter M. Fernandes Elmarie Myburgh Elizabeth A. Blackburn Ryan Ritchie Carol Austin Martin A. Wear Adrian J. Highton Andrew J. Keats Antonio Vong Jacqueline Dornan Jeremy C. Mottram Paul A. M. Michels Simon Pettit Malcolm D. Walkinshaw Fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice
description	Glycolytic enzymes are challenging drug targets due to their highly conserved active sites and phosphorylated substrates. Here, the authors identify fast acting allosteric inhibitors of Trypanosoma brucei phosphofructokinase that block trypanosome glycolysis and provide cure evidence in murine model.
format	article
author	Iain W. McNae James Kinkead Divya Malik Li-Hsuan Yen Martin K. Walker Chris Swain Scott P. Webster Nick Gray Peter M. Fernandes Elmarie Myburgh Elizabeth A. Blackburn Ryan Ritchie Carol Austin Martin A. Wear Adrian J. Highton Andrew J. Keats Antonio Vong Jacqueline Dornan Jeremy C. Mottram Paul A. M. Michels Simon Pettit Malcolm D. Walkinshaw
author_facet	Iain W. McNae James Kinkead Divya Malik Li-Hsuan Yen Martin K. Walker Chris Swain Scott P. Webster Nick Gray Peter M. Fernandes Elmarie Myburgh Elizabeth A. Blackburn Ryan Ritchie Carol Austin Martin A. Wear Adrian J. Highton Andrew J. Keats Antonio Vong Jacqueline Dornan Jeremy C. Mottram Paul A. M. Michels Simon Pettit Malcolm D. Walkinshaw
author_sort	Iain W. McNae
title	Fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice
title_short	Fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice
title_full	Fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice
title_fullStr	Fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice
title_full_unstemmed	Fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice
title_sort	fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute african trypanosomiasis in mice
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/4b5f2d939f554cc8b893fd1148232b4e
work_keys_str_mv	AT iainwmcnae fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT jameskinkead fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT divyamalik fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT lihsuanyen fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT martinkwalker fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT chrisswain fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT scottpwebster fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT nickgray fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT petermfernandes fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT elmariemyburgh fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT elizabethablackburn fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT ryanritchie fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT carolaustin fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT martinawear fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT adrianjhighton fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT andrewjkeats fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT antoniovong fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT jacquelinedornan fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT jeremycmottram fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT paulammichels fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT simonpettit fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice AT malcolmdwalkinshaw fastactingallostericphosphofructokinaseinhibitorsblocktrypanosomeglycolysisandcureacuteafricantrypanosomiasisinmice
_version_	1718394626322202624

Fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice

Ejemplares similares