Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1
Liu et al investigate the effects of divalent metal ions on catalysis and inhibition of the enzyme isocitrate dehydrogenase (IDH) and its cancer-linked variant R132H. They further identify the substrates for IDH as complexes with Mg2+ and show that allosteric inhibitors work by weakening Mg2+ bindin...
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2021
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oai:doaj.org-article:87f044b46ee747dba26b0e27f7cc54e62021-11-07T12:20:38ZRoles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 110.1038/s42003-021-02743-52399-3642https://doaj.org/article/87f044b46ee747dba26b0e27f7cc54e62021-11-01T00:00:00Zhttps://doi.org/10.1038/s42003-021-02743-5https://doaj.org/toc/2399-3642Liu et al investigate the effects of divalent metal ions on catalysis and inhibition of the enzyme isocitrate dehydrogenase (IDH) and its cancer-linked variant R132H. They further identify the substrates for IDH as complexes with Mg2+ and show that allosteric inhibitors work by weakening Mg2+ binding of R132H, providing mechanistic insights into the basis for selective R132H IDH1 inhibition.Shuang LiuMartine I. AbboudTobias JohnVictor MikhailovIngvild HvindenJohn Walsby-TickleXiao LiuIlaria PettinatiTom Cadoux-HudsonJames S. O. McCullaghChristopher J. SchofieldNature PortfolioarticleBiology (General)QH301-705.5ENCommunications Biology, Vol 4, Iss 1, Pp 1-16 (2021) |
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DOAJ |
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DOAJ |
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Biology (General) QH301-705.5 |
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Biology (General) QH301-705.5 Shuang Liu Martine I. Abboud Tobias John Victor Mikhailov Ingvild Hvinden John Walsby-Tickle Xiao Liu Ilaria Pettinati Tom Cadoux-Hudson James S. O. McCullagh Christopher J. Schofield Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1 |
description |
Liu et al investigate the effects of divalent metal ions on catalysis and inhibition of the enzyme isocitrate dehydrogenase (IDH) and its cancer-linked variant R132H. They further identify the substrates for IDH as complexes with Mg2+ and show that allosteric inhibitors work by weakening Mg2+ binding of R132H, providing mechanistic insights into the basis for selective R132H IDH1 inhibition. |
format |
article |
author |
Shuang Liu Martine I. Abboud Tobias John Victor Mikhailov Ingvild Hvinden John Walsby-Tickle Xiao Liu Ilaria Pettinati Tom Cadoux-Hudson James S. O. McCullagh Christopher J. Schofield |
author_facet |
Shuang Liu Martine I. Abboud Tobias John Victor Mikhailov Ingvild Hvinden John Walsby-Tickle Xiao Liu Ilaria Pettinati Tom Cadoux-Hudson James S. O. McCullagh Christopher J. Schofield |
author_sort |
Shuang Liu |
title |
Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1 |
title_short |
Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1 |
title_full |
Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1 |
title_fullStr |
Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1 |
title_full_unstemmed |
Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1 |
title_sort |
roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1 |
publisher |
Nature Portfolio |
publishDate |
2021 |
url |
https://doaj.org/article/87f044b46ee747dba26b0e27f7cc54e6 |
work_keys_str_mv |
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