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MeTC7 is a vitamin D receptor (VDR) antagonist (IC50 = 2.9 µM in a fluorescence polarization assay).1 It inhibits VDR transactivation in HEK293 cells (IC50 = 20.8 µM). It decreases the viability of OVCAR-8, OV-2008, SKOV3, Caov-3, and IGROV-1 ovarian cancer cells in a concentration-dependent manner. MeTC7 (250 nM) reduces retinoid X receptor α (RXRα) and importin-4 protein levels in OV-2008 cells. It decreases programmed cell death 1 ligand 1 (PD-L1) levels in primary human acute myeloid leukemia (AML) cells when used at a concentration of 500 nM.2 MeTC7 (10 mg/kg) reduces tumor growth in an SH-SY5Y neuroblastoma mouse xenograft model.1 Lipid nanoparticles (LNPs) containing MeTC7 selectively localize to the pancreas in mice.3
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1. Identification of a vitamin-
2. Vitamin D receptor antagonist MeTC7 inhibits PD-
3. Reengineering endogenous targeting lipid nanoparticles (ENDO) for systemic delivery of mRNA to pancreas. Adv. Mater. 37(40), e2507657 (2025).