Structure, function and small molecule modulation of intracellular sterol transport proteins

Laura Depta, Thomas Whitmarsh-Everiss, Luca Laraia*

*Corresponding author for this work

Research output: Contribution to journalReviewpeer-review

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Intracellular sterol transport proteins (STPs) are crucial for maintaining cellular lipid homeostasis by regulating local sterol pools. Despite structural similarities in their sterol binding domains, STPs have different substrate specificities, intracellular localisation and biological functions. In this review, we highlight recent advances in the determination of STP structures and how this regulates their lipid specificities. Furthermore, we cover the important discoveries relating to the intracellular localisation of STPs, and the organelles between which lipid transport is carried out, giving rise to specific functions in health and disease. Finally, serendipitous and targeted efforts to identify small molecule modulators of STPs, as well as their ability to act as tool compounds and potential therapeutics, will be discussed.
Original languageEnglish
Article number116856
JournalBioorganic and Medicinal Chemistry
Number of pages12
Publication statusPublished - 2022


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