Kawachi, Takashi and Tanaka, Shun and Fukuda, Akinori and Sumii, Yuji and Setiawan, Andi and Kotoku, Naoyuki and Kobayashi, Motomasa and Arai, Masayoshi Target Identification of the Marine Natural Products Dictyoceratin-A and -C as Selective Growth Inhibitors in Cancer Cells Adapted to Hypoxic Environments. MDPI Multidisciplinary Digital Publishing Institute.
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Abstract
Hypoxia-adapted cancer cells in tumors contribute to the pathological progression of cancer. The marine spongean sesquiterpene phenols dictyoceratin-A (1) and -C (2) have been shown to induce hypoxia-selective growth inhibition in cultured cancer cells and exhibit in vivo antitumor effects. These compounds inhibit the accumulation of hypoxia-inducible factor-1α (HIF-1α), which is a drug target in hypoxia-adapted cancer cells, under hypoxic conditions. However, the target molecules of compounds 1 and 2, which are responsible for decreasing HIF-1α expression under hypoxic conditions, remain unclear. In this study, we synthesized probe molecules for compounds 1 and 2 to identify their target molecules and found that both compounds bind to RNA polymerase II-associated protein 3 (RPAP3), which is a component of the R2TP/Prefoldin-like (PEDL) complex. In addition, RPAP3-knockdown cells showed a phenotype similar to that of compound-treated cells.
| Item Type: | Other |
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| Subjects: | Q Science > Q Science (General) |
| Depositing User: | Prof Andi Setiawan |
| Date Deposited: | 18 Feb 2022 01:19 |
| Last Modified: | 18 Feb 2022 01:19 |
| URI: | http://repository.lppm.unila.ac.id/id/eprint/39457 |
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