Hyperagonism of a Vitamin D Receptor Agonist/Histone Deacetylase Inhibitor Hybrid Molecule

1,25-Dihydroxyvitamin D (1,25D) analogs engage the vitamin D receptor (VDR) and can exert anticancer and immunomodulatory effects. Although tumors often resist 1,25D monotherapy, combining VDR agonism with histone deacetylase inhibitors (HDACi) restores anticancer efficacy. Here, we present AC-340,...

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التفاصيل البيبلوغرافية
المؤلف الرئيسي:	Fatemeh Sarmadi (18865539) (author)
مؤلفون آخرون:	Amelia Caza (22273467) (author), Zhizhong Gao (18865542) (author), Natacha Rochel (225991) (author), James L. Gleason (1853971) (author), John H. White (63329) (author)
منشور في:	2025
الموضوعات:	Biophysics Biochemistry Medicine Cell Biology Genetics Molecular Biology Pharmacology Developmental Biology Cancer Virology Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified novel bifunctional molecule multiple melanoma models multiple cancer models histone deacetylase inhibitors elevated h3k27 acetylation comparative structural studies restores anticancer efficacy vdr target genes combining vdr agonism vdr agonist backbone 340 hdaci activity exert anticancer vdr hyperagonist robust bifunctionality rnaseq analysis receptor agonist qpcr revealed likely coupled incorporates hdaci immunomodulatory effects combination therapies coactivator cbp broad array analogs engage active transcription 340 superinduces 340 functions 340 forms
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Hyperagonism of a Vitamin D Receptor Agonist/Histone Deacetylase Inhibitor Hybrid Molecule

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