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Biomolecules, Volume 14, Issue 3
March 2024 - 139 articles
Cover Story: Orphan nuclear receptor 4A1 (NR4A1, Nur77) and NR4A2 (Nurr1) are pro-oncogenic factors in solid tumors. A recent study reported that a series of 1,1-bis(3′-indoly)-1-(3,5-disubstitutedphenyl)methane (DIM-3,5) analogs were potent inhibitors of mammary tumor growth in a mouse xenograft model. The potency of these compounds coupled with >60% similarity of the ligand binding domains of NR4A1 and NR4A2 suggested that DIM-3,5 compounds may also bind and activate NR4A2. This study demonstrates that DIM-3,5 analogs bind both receptors as novel dual NR4A1/NR4A2 ligands that act as inverse NR4A1/2 agonists in cancer cell lines. These compounds will be used to target tumors and tumor-infiltrating lymphocytes. View this paper
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Biomolecules - ISSN 2218-273XCreative Common CC BY license