کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1368588 | 981704 | 2016 | 5 صفحه PDF | دانلود رایگان |
The steroidogenic enzyme 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) is a therapeutic target in the management of androgen-sensitive diseases such as prostate cancer and benign prostate hyperplasia. In this Letter, we designed and synthesized the first fluorescent inhibitor of this enzyme by combining a fluorogenic dansyl moiety to the chemical structure of a known inhibitor of 17β-HSD3. The synthesized compound 3 is a potent fluorogenic compound (λex = 348 nm and λem = 498 nm). It crosses the cell membrane, keeps its fluorescent properties and is distributed inside the LNCaP cells overexpressing 17β-HSD3, where it inhibits the transformation of 4-androstene-3,17-dione into the androgen testosterone (IC50 = 262 nM).
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 9, 1 May 2016, Pages 2179–2183