关于前核苷酸方法在抗病毒化疗中潜力的新见解。

New insights regarding the potential of the pronucleotide approach in antiviral chemotherapy.

作者信息

Gosselin G, Girardet J L, Périgaud C, Benzaria S, Lefebvre I, Schlienger N, Pompon A, Imbach J L

机构信息

Laboratoire de Chimie Bioorganique, URA CNRS 488, Université de Montpellier II, France.

出版信息

Acta Biochim Pol. 1996;43(1):196-208.

PMID:8790724

Abstract

The rationale for a pronucleotide approach based on the use of phosphotriesters which incorporate enzyme-mediated bio-labile protection is discussed in detail. Among the studied bio-labile phosphate protecting groups, the S-acyl-2-thioethyl (SATE) groups appeared the most promising as exemplified in cell culture systems in the case of the pronucleotides of 3'-azido-3'-deoxythymidine, 2',3'-didehydro-3'-deoxythymidine, 2',3'-dideoxyadenosine and acyclovir In vivo implementations of such bis(SATE) pronucleotides have been planned for future animal studies.

摘要

详细讨论了基于使用包含酶介导的生物可裂解保护的磷酸三酯的前核苷酸方法的基本原理。在所研究的生物可裂解磷酸保护基团中，S-酰基-2-硫代乙基（SATE）基团似乎最有前景，如在细胞培养系统中3'-叠氮基-3'-脱氧胸苷、2'，3'-二脱氢-3'-脱氧胸苷、2'，3'-二脱氧腺苷和阿昔洛韦的前核苷酸所示。已经计划在未来的动物研究中对这种双（SATE）前核苷酸进行体内应用。