Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.

Marc Lamblin,Basel Dabbas,Russell Spingarn,Rodrigo Mendoza-Sanchez,Tian-Tian Wang,Beum-Soo An,Dao Chao Huang,Richard Kremer,John H White,James L Gleason

Bioorganic & Medicinal Chemistry（2010）

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摘要

Incorporation of zinc-binding groups into the side-chain of 1α,25-dihydroxyvitamin D3 (1,25D) fully bifunctional hybrid molecules which act both as vitamin D receptor agonists and histone deacetylase inhibitors. These bifunctional hybrids display in vitro antiproliferative activity against the AT84 squamous carcinoma cell line while lacking the in vivo hypercalcemic effects of 1,25D.

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关键词

Vitamin D,Vitamin D receptor (VDR),VDR agonists,Histone deacetylases (HDACs),HDAC inhibitors,Transcriptional regulation,Zinc-binding groups,Hybrid molecules,Dual pharmacophores

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