Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase

Squalene epoxidase (SQLE) is a key enzyme in cholesterol biosynthesis and is a target for hypercholesteremia and cancer drug development. Here the authors present the crystal structures of the human SQLE catalytic domain alone and bound with small molecule inhibitors, which will facilitate the devel...

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Autores principales: Anil K. Padyana, Stefan Gross, Lei Jin, Giovanni Cianchetta, Rohini Narayanaswamy, Feng Wang, Rui Wang, Cheng Fang, Xiaobing Lv, Scott A. Biller, Lenny Dang, Christopher E. Mahoney, Nelamangala Nagaraja, David Pirman, Zhihua Sui, Janeta Popovici-Muller, Gromoslaw A. Smolen
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Publicado: Nature Portfolio 2019
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Acceso en línea:https://doaj.org/article/13114a6254b94cd5a8f05eeabf842c50
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spelling oai:doaj.org-article:13114a6254b94cd5a8f05eeabf842c502021-12-02T17:01:40ZStructure and inhibition mechanism of the catalytic domain of human squalene epoxidase10.1038/s41467-018-07928-x2041-1723https://doaj.org/article/13114a6254b94cd5a8f05eeabf842c502019-01-01T00:00:00Zhttps://doi.org/10.1038/s41467-018-07928-xhttps://doaj.org/toc/2041-1723Squalene epoxidase (SQLE) is a key enzyme in cholesterol biosynthesis and is a target for hypercholesteremia and cancer drug development. Here the authors present the crystal structures of the human SQLE catalytic domain alone and bound with small molecule inhibitors, which will facilitate the development of next-generation SQLE inhibitors.Anil K. PadyanaStefan GrossLei JinGiovanni CianchettaRohini NarayanaswamyFeng WangRui WangCheng FangXiaobing LvScott A. BillerLenny DangChristopher E. MahoneyNelamangala NagarajaDavid PirmanZhihua SuiJaneta Popovici-MullerGromoslaw A. SmolenNature PortfolioarticleScienceQENNature Communications, Vol 10, Iss 1, Pp 1-10 (2019)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Anil K. Padyana
Stefan Gross
Lei Jin
Giovanni Cianchetta
Rohini Narayanaswamy
Feng Wang
Rui Wang
Cheng Fang
Xiaobing Lv
Scott A. Biller
Lenny Dang
Christopher E. Mahoney
Nelamangala Nagaraja
David Pirman
Zhihua Sui
Janeta Popovici-Muller
Gromoslaw A. Smolen
Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase
description Squalene epoxidase (SQLE) is a key enzyme in cholesterol biosynthesis and is a target for hypercholesteremia and cancer drug development. Here the authors present the crystal structures of the human SQLE catalytic domain alone and bound with small molecule inhibitors, which will facilitate the development of next-generation SQLE inhibitors.
format article
author Anil K. Padyana
Stefan Gross
Lei Jin
Giovanni Cianchetta
Rohini Narayanaswamy
Feng Wang
Rui Wang
Cheng Fang
Xiaobing Lv
Scott A. Biller
Lenny Dang
Christopher E. Mahoney
Nelamangala Nagaraja
David Pirman
Zhihua Sui
Janeta Popovici-Muller
Gromoslaw A. Smolen
author_facet Anil K. Padyana
Stefan Gross
Lei Jin
Giovanni Cianchetta
Rohini Narayanaswamy
Feng Wang
Rui Wang
Cheng Fang
Xiaobing Lv
Scott A. Biller
Lenny Dang
Christopher E. Mahoney
Nelamangala Nagaraja
David Pirman
Zhihua Sui
Janeta Popovici-Muller
Gromoslaw A. Smolen
author_sort Anil K. Padyana
title Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase
title_short Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase
title_full Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase
title_fullStr Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase
title_full_unstemmed Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase
title_sort structure and inhibition mechanism of the catalytic domain of human squalene epoxidase
publisher Nature Portfolio
publishDate 2019
url https://doaj.org/article/13114a6254b94cd5a8f05eeabf842c50
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