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Endogenous and fluorescent sterols reveal the molecular basis for ligand selectivity of human sterol transporters.
Depta, Laura; Bryce-Rogers, Hogan P; Dekker, Nienke J; Bønke, Anna Wiehl; Camporese, Nicolo'; Qian, Mingxing; Xu, Yuanjian; Covey, Douglas F; Laraia, Luca.
Afiliación
  • Depta L; Department of Chemistry, Technical University of Denmark Kemitorvet 207, 2800 Kongens Lyngby, Denmark.
  • Bryce-Rogers HP; Department of Chemistry, Technical University of Denmark Kemitorvet 207, 2800 Kongens Lyngby, Denmark.
  • Dekker NJ; Department of Chemistry, Technical University of Denmark Kemitorvet 207, 2800 Kongens Lyngby, Denmark.
  • Bønke AW; Department of Chemistry, Technical University of Denmark Kemitorvet 207, 2800 Kongens Lyngby, Denmark.
  • Camporese N; Department of Chemistry, Technical University of Denmark Kemitorvet 207, 2800 Kongens Lyngby, Denmark.
  • Qian M; Department of Developmental Biology, Washington University in St. Louis, School of Medicine, St. Louis, MO 63110.
  • Xu Y; Taylor Family Institute for Innovative Psychiatric Research, Washington University in St. Louis, School of Medicine, St. Louis, MO 63110.
  • Covey DF; Department of Developmental Biology, Washington University in St. Louis, School of Medicine, St. Louis, MO 63110.
  • Laraia L; Taylor Family Institute for Innovative Psychiatric Research, Washington University in St. Louis, School of Medicine, St. Louis, MO 63110.
bioRxiv ; 2024 Jul 22.
Article en En | MEDLINE | ID: mdl-39091845
ABSTRACT
Sterol transport proteins (STPs) play a pivotal role in cholesterol homeostasis and therefore are essential for healthy human physiology. Despite recent advances in dissecting functions of STPs in the human cell, there is still a significant knowledge gap regarding their specific biological functions and a lack of suitable selective probes for their study. Here, we profile fluorescent steroid-based probes across ten STPs, uncovering substantial differences in their selectivity, aiding the retrospective and prospective interpretation of biological results generated with those probes. These results guided the establishment of an STP screening panel combining diverse biophysical assays, enabling the evaluation of 41 steroid-based natural products and derivatives. Combining this with a thorough structural analysis revealed the molecular basis for STP specific selectivity profiles, leading to the uncovering of several new potent and selective Aster-B inhibitors, and supporting the role of this protein in steroidogenesis.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: BioRxiv Año: 2024 Tipo del documento: Article País de afiliación: Dinamarca Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: BioRxiv Año: 2024 Tipo del documento: Article País de afiliación: Dinamarca Pais de publicación: Estados Unidos