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组蛋白脱乙酰酶 8 (HDAC8) 的选择性抑制剂
由Suzuki, Miyata等人研发出的N-Hydroxy-3-[1-(phenylthio)methyl-1H-1,2,3-triazol-4-yl]benzamide (NCC-149)，可选择性抑制组蛋白脱乙酰酶 8 (HDAC8)。组蛋白脱乙酰酶 (HDAC)可以调控基因表达，例如肿瘤抑制基因，通过催化组蛋白中的赖氨酸残基的脱乙酰反应实现调控。据报道，组蛋白脱乙酰酶的一种同种型—HDAC8与T细胞淋巴瘤和神经母细胞瘤的肿瘤发生有关。由于NCC-149对HDAC8和肿瘤细胞的生长具有选择性抑制活性，预计它将用作试验胚胎学的研究工具和抗癌药。
文献
- 1) T. Suzuki, Y. Ota, Y. Kasuya, M. Mutsuga, Y. Kawamura, H. Tsumoto, H. Nakagawa, M. G. Finn, N. Miyata, Angew. Chem. Int. Ed. 2010, 49, 6817.
- 2) T. Suzuki, Y. Ota, M. Ri , M. Bando, A. Gotoh, Y. Itoh, H. Tsumoto, P. R. Tatum, T. Mizukami, H. Nakagawa, S. Iida, R. Ueda, K. Shirahige, N. Miyata, J. Med. Chem. 2012, 55, 9562.