Oligonucleotide-based telomerase inhibitors with a photoresponsive α-chloroaldehyde.

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Tác giả: Kentaro Kobata, Akio Kobori, Kazuki Matsubara, Kazuya Matsuo, Yuki Narita, Risa Nishikawa, Tomonori Waku

Ngôn ngữ: eng

Ký hiệu phân loại: 133.594 Types or schools of astrology originating in or associated with a

Thông tin xuất bản: England : Bioorganic & medicinal chemistry letters , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 691482

Telomerase, a ribonucleoprotein, is a reverse transcriptase that uses telomerase RNA component (hTR) as a template to elongate telomeric DNA at the ends of chromosomes. This enzyme plays a critical role in oncogenic cellular transformation. Therefore, the telomerase is considered an attractive target for cancer therapy. In this study, we synthesized photo-cross-linking oligodeoxyribonucleotides (ODNs) with a photoresponsive α-chloroaldehyde (PCA) moiety at the 3'-end or the 5'-end of the ODNs and evaluated the inhibition efficiencies for telomerase activity. PCA-modified ODNs with a sequence complementary to the template RNA of telomerase inhibited telomerase activity upon UV irradiation, whereas those with scramble sequence showed no significant inhibition. The 50 % inhibitory concentration (IC
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