Structural insights into the inhibition mechanism of human sterol O-acyltransferase 1 by a competitive inhibitor

Chengcheng Guan; Yange Niu; Si-Cong Chen; Yunlu Kang; Jing-Xiang Wu; Koji Nishi; Catherine C. Y. Chang; Ta-Yuan Chang; Tuoping Luo; Lei Chen

doi:10.1038/s41467-020-16288-4

Nature Communications (May 2020)

Structural insights into the inhibition mechanism of human sterol O-acyltransferase 1 by a competitive inhibitor

Chengcheng Guan,
Yange Niu,
Si-Cong Chen,
Yunlu Kang,
Jing-Xiang Wu,
Koji Nishi,
Catherine C. Y. Chang,
Ta-Yuan Chang,
Tuoping Luo,
Lei Chen

Affiliations

Chengcheng Guan: State Key Laboratory of Membrane Biology, Institute of Molecular Medicine, Peking University, Beijing Key Laboratory of Cardiometabolic Molecular Medicine
Yange Niu: State Key Laboratory of Membrane Biology, Institute of Molecular Medicine, Peking University, Beijing Key Laboratory of Cardiometabolic Molecular Medicine
Si-Cong Chen: Key Laboratory of Bioorganic Chemistry and Molecular Engineering, Ministry of Education and Beijing National Laboratory for Molecular Science, College of Chemistry and Molecular Engineering, Peking University
Yunlu Kang: State Key Laboratory of Membrane Biology, Institute of Molecular Medicine, Peking University, Beijing Key Laboratory of Cardiometabolic Molecular Medicine
Jing-Xiang Wu: State Key Laboratory of Membrane Biology, Institute of Molecular Medicine, Peking University, Beijing Key Laboratory of Cardiometabolic Molecular Medicine
Koji Nishi: Department of Biochemistry and Cell Biology, Geisel School of Medicine at Dartmouth
Catherine C. Y. Chang: Department of Biochemistry and Cell Biology, Geisel School of Medicine at Dartmouth
Ta-Yuan Chang: Department of Biochemistry and Cell Biology, Geisel School of Medicine at Dartmouth
Tuoping Luo: Key Laboratory of Bioorganic Chemistry and Molecular Engineering, Ministry of Education and Beijing National Laboratory for Molecular Science, College of Chemistry and Molecular Engineering, Peking University
Lei Chen: State Key Laboratory of Membrane Biology, Institute of Molecular Medicine, Peking University, Beijing Key Laboratory of Cardiometabolic Molecular Medicine

DOI: https://doi.org/10.1038/s41467-020-16288-4
Journal volume & issue: Vol. 11, no. 1
pp. 1 – 11

Abstract

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Sterol O-acyltransferase 1 (SOAT1, also named ACAT1) is an endoplasmic reticulum resident enzyme which catalyzes the esterification of cholesterol to generate cholesteryl esters. Here, authors report cryo-EM structures of human SOAT1 which reveal the binding site of the competitive inhibitor CI-976.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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