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Enhanced Th9-Mediated Adoptive Cell Therapy Against Mouse Melanoma Through GPR34/LPS1 Inverse Agonist Modulation
Inhibition of cannabinoid receptor 1 (CB1) has shown efficacy in reducing body weight and improving metabolic parameters, with the effects correlating with target engagement in the brain. Recently, the peripheral effects of inhibiting the CB1 receptor has been appreciated through studies in diet-ind...
ORGANISM(S): Mus musculus 
Genome-wide occupancy of PPARG and RXRA after treatment with PPARG inverse agonist
Liver-specific LXR inverse agonist restores lipid homeostasis in animal models and humans
Th9 is a relatively new type of CD4+ T-cell subset that exhibits stronger anti-tumor immunity compared to other Th cell subsets. However, the potential of Th9-based adoptive cell therapy (ACT) is largely constrained by its low differentiation efficiency and short-lived nature. GPR34 (also known as L...
ORGANISM(S): Mus musculus 
2026-09-30 | GSE286878 | GEO
Peroxisome proliferator-activated receptor gamma (PPARγ) is a validated therapeutic target for type 2 diabetes (T2D), but current FDA-approved agonists such as the glitazones are limited by adverse effects. SR10171, a non-covalent partial inverse agonist with modest binding potency, improves insulin...
ORGANISM(S): Homo sapiens (Human) 
2025-11-15 | PXD066095 | Pride
Work published by Wang et al. described pharmacological inhibition of RORg with an inverse agonist (SR2211) which led to a decrease in AR gene expression and a reduction in AR protein, which led to the loss of an AR gene expression signature. We have developed a novel, specific, RORg inverse agonist...
ORGANISM(S): Homo sapiens 
We report our mechanistic investigation into the conformationally-driven activation bias of PPARG in muscle-invasive urothelial cancer (MIUC) and our efforts to pharmacologically reverse this activation bias through covalent PPARG inverse agonism. Studies into tumor-associated mutations in both PPAR...
ORGANISM(S): Homo sapiens 
2026-05-28 | GSE298628 | GEO
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