H-phosphonate derivatives as novel peptide deformylase inhibitors.
H-phosphonate derivatives as novel peptide deformylase inhibitors.
复制标题
H-膦酸酯衍生物作为新型肽去甲酰基酶抑制剂。
DOI：
10.1016/s0960-894x(98)00443-0
复制
发表时间：
1998
影响因子：
2.7
通讯作者：
Pei,D
中科院分区：
文献类型：
--
作者：
Hu,YJ;Rajagopalan,PT;Pei,D
肽脱甲酰基酶在原核生物蛋白质成熟过程中催化从新生多肽中去除N-末端甲酰基，是细菌生存所必需的。它在真核生物中的缺失使其成为设计新型抗菌剂的一个有吸引力的靶点。合成了具有竞争性的脱甲酰基酶抑制剂--肽基H-膦。
Peptide deformylase catalyzes the removal of the N-terminal formyl group from nascent polypeptides during prokaryotic protein maturation and is essential for bacterial survival. Its absence from eukaryotic organisms makes it an attractive target for designing novel antibacterial agents. Peptidyl H-phosphonates were synthesized and shown to be competitive inhibitors of the deformylase.