Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer

While biologics have been successfully applied in TNF antagonist treatments, there are no clinically approved small molecules that target TNF. Here, the authors discover potent small molecule inhibitors of TNF, elucidate their molecular mechanism, and demonstrate TNF inhibition in vitro and in vivo.

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Autores principales:	James O’Connell, John Porter, Boris Kroeplien, Tim Norman, Stephen Rapecki, Rachel Davis, David McMillan, Tracy Arakaki, Alex Burgin, David Fox III, Tom Ceska, Fabien Lecomte, Alison Maloney, Alex Vugler, Bruce Carrington, Benjamin P Cossins, Tim Bourne, Alastair Lawson
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2019
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/cd8aea08c83948d3a69fc5302494dedc
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spelling	oai:doaj.org-article:cd8aea08c83948d3a69fc5302494dedc2021-12-02T17:01:34ZSmall molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer10.1038/s41467-019-13616-12041-1723https://doaj.org/article/cd8aea08c83948d3a69fc5302494dedc2019-12-01T00:00:00Zhttps://doi.org/10.1038/s41467-019-13616-1https://doaj.org/toc/2041-1723While biologics have been successfully applied in TNF antagonist treatments, there are no clinically approved small molecules that target TNF. Here, the authors discover potent small molecule inhibitors of TNF, elucidate their molecular mechanism, and demonstrate TNF inhibition in vitro and in vivo.James O’ConnellJohn PorterBoris KroeplienTim NormanStephen RapeckiRachel DavisDavid McMillanTracy ArakakiAlex BurginDavid Fox IIITom CeskaFabien LecomteAlison MaloneyAlex VuglerBruce CarringtonBenjamin P CossinsTim BourneAlastair LawsonNature PortfolioarticleScienceQENNature Communications, Vol 10, Iss 1, Pp 1-12 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q James O’Connell John Porter Boris Kroeplien Tim Norman Stephen Rapecki Rachel Davis David McMillan Tracy Arakaki Alex Burgin David Fox III Tom Ceska Fabien Lecomte Alison Maloney Alex Vugler Bruce Carrington Benjamin P Cossins Tim Bourne Alastair Lawson Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer
description	While biologics have been successfully applied in TNF antagonist treatments, there are no clinically approved small molecules that target TNF. Here, the authors discover potent small molecule inhibitors of TNF, elucidate their molecular mechanism, and demonstrate TNF inhibition in vitro and in vivo.
format	article
author	James O’Connell John Porter Boris Kroeplien Tim Norman Stephen Rapecki Rachel Davis David McMillan Tracy Arakaki Alex Burgin David Fox III Tom Ceska Fabien Lecomte Alison Maloney Alex Vugler Bruce Carrington Benjamin P Cossins Tim Bourne Alastair Lawson
author_facet	James O’Connell John Porter Boris Kroeplien Tim Norman Stephen Rapecki Rachel Davis David McMillan Tracy Arakaki Alex Burgin David Fox III Tom Ceska Fabien Lecomte Alison Maloney Alex Vugler Bruce Carrington Benjamin P Cossins Tim Bourne Alastair Lawson
author_sort	James O’Connell
title	Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer
title_short	Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer
title_full	Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer
title_fullStr	Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer
title_full_unstemmed	Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer
title_sort	small molecules that inhibit tnf signalling by stabilising an asymmetric form of the trimer
publisher	Nature Portfolio
publishDate	2019
url	https://doaj.org/article/cd8aea08c83948d3a69fc5302494dedc
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Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer

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