Tailoring FXR Modulators for Intestinal Specificity: Recent Progress and Insights

Amanda Morrison; Bahaa Elgendy

doi:10.3390/molecules29092022

Tailoring FXR Modulators for Intestinal Specificity: Recent Progress and Insights

Research output: Contribution to journal › Review article › peer-review

Abstract

While FXR has shown promise in regulating bile acid synthesis and maintaining glucose and lipid homeostasis, undesired side effects have been observed in clinical trials. To address this issue, the development of intestinally restricted FXR modulators has gained attention as a new avenue for drug design with the potential for safer systematic effects. Our review examines all currently known intestinally restricted FXR ligands and provides insights into the steps taken to enhance intestinal selectivity.

Original language	English
Article number	2022
Journal	Molecules
Volume	29
Issue number	9
DOIs	https://doi.org/10.3390/molecules29092022
State	Published - May 2024

Keywords

bile acid synthesis
drug design
farnesoid X receptor (FXR)
intestinal selectivity
metabolic diseases

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10.3390/molecules29092022

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abstract = "While FXR has shown promise in regulating bile acid synthesis and maintaining glucose and lipid homeostasis, undesired side effects have been observed in clinical trials. To address this issue, the development of intestinally restricted FXR modulators has gained attention as a new avenue for drug design with the potential for safer systematic effects. Our review examines all currently known intestinally restricted FXR ligands and provides insights into the steps taken to enhance intestinal selectivity.",

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author = "Amanda Morrison and Bahaa Elgendy",

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KW - drug design

KW - farnesoid X receptor (FXR)

KW - intestinal selectivity

KW - metabolic diseases

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Tailoring FXR Modulators for Intestinal Specificity: Recent Progress and Insights

Abstract

Keywords

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