Hydrophobicity-oriented drug design (HODD) of new human 4-hydroxyphenylpyruvate dioxygenase inhibitors
Hydrophobicity-oriented drug design (HODD) of new human 4-hydroxyphenylpyruvate dioxygenase inhibitors
复制标题
新型人4-羟苯基丙酮酸双加氧酶抑制剂的疏水性药物设计（HODD）
DOI：
10.1016/j.ejmech.2019.01.032
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发表时间：
2019
影响因子：
6.7
通讯作者：
Yang Guang-Fu
中科院分区：
文献类型：
--
作者：
Ndikuryayo Ferdin;Kang Wei-Ming;Wu Feng-Xu;Yang Wen-Chao;Yang Guang-Fu
Involved in the tyrosine degradation pathway, 4-hydroxyphenylpyruvate dioxygenase (HPPD) is an important target for treating type I tyrosinemia. To discover novel HPPD inhibitors, we proposed a hydrophobicity-oriented drug design (HODD) strategy based on the interactions between HPPD and the commercial drug NTBC. Most of the new compounds showed improved activity, compoundd23being the most active candidate (IC50= 0.047 μM) with about 2-fold more potent than NTBC (IC50= 0.085 μM). Therefore, compoundd23is a potential drug candidate to treat type I tyrosinemia.
