Tailoring FXR Modulators for Intestinal Specificity: Recent Progress and Insights
Amanda Maria Morrison, Bahaa Elgendy
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.
Topics & Concepts
Farnesoid X receptorBile acidComputational biologyChemistryPharmacologyBiologyNuclear receptorBiochemistryTranscription factorGeneDrug Transport and Resistance MechanismsPediatric Hepatobiliary Diseases and TreatmentsLiver Disease Diagnosis and Treatment