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The 2',3'-dideoxyriboside of 2,6-diaminopurine and its 2',3'-didehydro derivative inhibit the deamination of 2',3'-dideoxyadenosine, an inhibitor of human immunodeficiency virus (HIV) replication.

作者信息

Balzarini J, Robins M J, Zou R M, Herdewijn P, De Clercq E

出版信息

Biochem Biophys Res Commun. 1987 May 29;145(1):277-83. doi: 10.1016/0006-291x(87)91317-9.

DOI:10.1016/0006-291x(87)91317-9
PMID:3496090
Abstract

The 2',3'-dideoxyriboside of 2,6-diaminopurine (ddDAPR) and its 2',3'-didehydro derivative (ddeDAPR) are poor substrates for adenosine deaminase (ADA) but potent inhibitors of the enzyme. Their Km values for ADA are of the same order of magnitude as those of the natural adenosine (Ado) and 2'-deoxyadenosine (dAdo), but their Vmax values are 35-fold (ddDAPR) to 350-fold (ddeDAPR) lower than those of Ado and dAdo. The Ki/K values of ADA for ddeDAPR (as inhibitor) and Ado, 2',3'-dideoxyadenosine (ddAdo) and 9-beta-D-arabinofuranosyladenine (araA) as the substrates are 0.17, 0.05 and 0.06, respectively. ddDAPR is about 3-fold less potent as an inhibitor of ADA than ddeDAPR. The 2,6-diaminopurine derivatives ddeDAPR and ddDAPR [which is also a potent inhibitor of human immunodeficiency virus (HIV)], may hold great promise, from a chemotherapeutic viewpoint, in combination with other adenosine analogues such as ddAdo and araA, which have been recognized and/or being pursued as either anti-retrovirus or anti-herpesvirus agents.

摘要

相似文献

1
The 2',3'-dideoxyriboside of 2,6-diaminopurine and its 2',3'-didehydro derivative inhibit the deamination of 2',3'-dideoxyadenosine, an inhibitor of human immunodeficiency virus (HIV) replication.
Biochem Biophys Res Commun. 1987 May 29;145(1):277-83. doi: 10.1016/0006-291x(87)91317-9.
2
The 2',3'-dideoxyriboside of 2,6-diaminopurine selectively inhibits human immunodeficiency virus (HIV) replication in vitro.2,6-二氨基嘌呤的2',3'-二脱氧核糖核苷在体外能选择性抑制人类免疫缺陷病毒（HIV）的复制。
Biochem Biophys Res Commun. 1987 May 29;145(1):269-76. doi: 10.1016/0006-291x(87)91316-7.
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