双（SATE）磷酸三酯ddA和3'-叠氮基-2'，3'-双脱氧胸苷对人类免疫缺陷病毒在人T细胞培养物中的复制具有同等抑制作用。
Equal inhibition of the replication of human immunodeficiency virus in human T-cell culture by ddA bis(SATE)phosphotriester and 3'-azido-2',3'-dideoxythymidine.
作者信息
Perigaud C, Aubertin A M, Benzaria S, Pelicano H, Girardet J L, Maury G, Gosselin G, Kirn A, Imbach J L
机构信息
Laboratoire de Chimie Bio-Organique, U.R.A. 488 du C.N.R.S., Université de Montpellier II, France.
出版信息
Biochem Pharmacol. 1994 Jul 5;48(1):11-14. doi: 10.1016/0006-2952(94)90217-8.
It is shown that ddA bis(SATE)phosphotriester is one of the most potent anti-HIV agents in cell culture. Compared with the parent nucleoside, ddA, an increase of 3 orders of magnitude was observed in the EC50, which makes this compound as active as AZT. This can be tentatively explained if one considers that direct ddAMP intracellular delivery shunts the well established ddA/ddI metabolism pathway.
结果表明，双（SATE）磷酸三酯双脱氧腺苷（ddA bis(SATE)phosphotriester）是细胞培养中最有效的抗HIV药物之一。与母体核苷双脱氧腺苷（ddA）相比，其半数有效浓度（EC50）增加了3个数量级，这使得该化合物与齐多夫定（AZT）一样具有活性。如果考虑到直接的双脱氧腺苷一磷酸（ddAMP）细胞内递送绕过了已确立的双脱氧腺苷/双脱氧肌苷（ddA/ddI）代谢途径，这一点可以得到初步解释。
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