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

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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Bibliographic Details
Main Author: Fatemeh Sarmadi (18865539) (author)
Other Authors: Amelia Caza (22273467) (author), Zhizhong Gao (18865542) (author), Natacha Rochel (225991) (author), James L. Gleason (1853971) (author), John H. White (63329) (author)
Published: 2025
Subjects:
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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