Targeting Nuclear Receptors in Research

The FXR activator GW 40644 [27 (link)], as well as Z-Guggulsterone, an inhibitor of FXR transactivation, were used to target FXR [30 (link)]. RG-239, a 3β-allyl semisynthetic derivative of betallinic acid, was used as a selective TGR5 activator [29 (link)]. The dual FXR/TGR5 ligand obeticholic acid (INT 747) [15 (link)] was also used. To target the liver X receptor (LXR), the LXRα agonist WAY 252623 [75 (link)] and LXRα antagonist GSK2033 [31 (link)] were used.

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Ackerman H.D, & Gerhard G.S. (2023). Bile Acids Induce Neurite Outgrowth in Nsc-34 Cells via TGR5 and a Distinct Transcriptional Profile. Pharmaceuticals, 16(2), 174.

Publication 2023

Acid Gsk2033 Int 747 Ligand Liver x receptor Obeticholic acid Transactivation Way 252623 Z guggulsterone

Corresponding Organization : Temple University

Other organizations : Moffitt Cancer Center, Molecular Oncology (United States)

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Variable analysis

independent variables

GW 40644 (FXR activator)
Z-Guggulsterone (FXR transactivation inhibitor)
RG-239 (TGR5 activator)
Obeticholic acid (INT 747) (dual FXR/TGR5 ligand)
WAY 252623 (LXRα agonist)
GSK2033 (LXRα antagonist)

dependent variables

Not explicitly mentioned

control variables

Not explicitly mentioned

controls

Positive control: Not specified
Negative control: Not specified

Annotations

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