鉴定含有羟甲基羰基（HMC）电子等排体作为过渡态模拟物的拟肽类人嗜T淋巴细胞病毒I型蛋白酶抑制剂。
Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic.
作者信息
Maegawa Hikoichiro, Kimura Tooru, Arii Yasuhiro, Matsui Yasuko, Kasai Soko, Hayashi Yoshio, Kiso Yoshiaki
机构信息
Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
出版信息
Bioorg Med Chem Lett. 2004 Dec 6;14(23):5925-9. doi: 10.1016/j.bmcl.2004.09.034.
Towards the development of chemotherapy for the infection by human T-cell leukemia virus type I (HTLV-I), we have established evaluation systems for HTLV-I protease (PR) inhibitors using both recombinant and chemically synthesized HTLV-I PRs. Newly synthesized substrate-based inhibitors containing hydroxymethylcarbonyl (HMC) isostere showed potent anti-HTLV-I PR activity.
为了开发针对人类I型T细胞白血病病毒（HTLV-I）感染的化疗方法，我们利用重组和化学合成的HTLV-I蛋白酶（PR）建立了HTLV-I PR抑制剂的评估系统。新合成的含羟甲基羰基（HMC）等排体的基于底物的抑制剂显示出强大的抗HTLV-I PR活性。
Zotero 插件