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
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2019
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Acceso en línea:https://doaj.org/article/13114a6254b94cd5a8f05eeabf842c50
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Sumario: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.