Article ID Journal Published Year Pages File Type
10593525 Bioorganic & Medicinal Chemistry Letters 2013 5 Pages PDF
Abstract
We synthesized stapled helical leucine-based peptides (DPI-01-07) containing 2-aminoisobutyric acid and a covalent cross-linked unit as inhibitors of vitamin D receptor (VDR)-coactivator interactions. The effects of these peptides on the human VDR were examined in an inhibition assay based on the receptor cofactor assay system, and one of them, DPI-07, exhibited potent inhibitory activity (IC50: 3.2 μM).
Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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