IN-VITRO ANTI-HIV-1 ACTIVITY OF HIV PROTEASE INHIBITOR KNI-272 IN RESTING AND ACTIVATED CELLS - IMPLICATIONS FOR ITS COMBINED USE WITH AZT OR DDI

被引：10

作者：

CHOKEKIJCHAI, S

SHIRASAKA, T

WEINSTEIN, JN

MITSUYA, H

机构：

[1] NCI,MED BRANCH,EXPTL RETROVIROL SECT,BETHESDA,MD 20892

[2] NCI,THEORET IMMUNOL SECT,MATH BIOL LAB,BETHESDA,MD 20892

来源：

ANTIVIRAL RESEARCH | 1995年 / 28卷 / 01期

关键词：

ACQUIRED IMMUNODEFICIENCY SYNDROME (AIDS); ANTIVIRAL THERAPY; AZIDOTHYMIDINE; DIDEOXYINOSINE; PROTEASE INHIBITOR; COMBINATION THERAPY;

D O I：

10.1016/0166-3542(95)00036-L

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

KNI-272, a conformationally constrained human immunodeficiency virus (HIV) protease inhibitor containing a P1 allophenylnorstatine (Apns) ((2S,3S)- 3-amino-2-hydroxy-4-phenylbutyric acid), has been shown to be a selective and potent inhibitor of the replication of a wide spectrum of HIV strains in vitro. When KNI-272 was tested in combination with 3'-azido-2',3'-dideoxythymidine (AZT) or 2',3'-dideoxyinosine (ddI) against a primary HIV-1 isolate in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBM), its activity was identified to be additive, but not synergistic or antagonistic, as analyzed with the COMBO program package. When tested alone for anti-HIV-1 activity in resting PBM (R-PBM) and PHA-PBM, KNI-272 was found to be comparably potent against the virus in both target cell populations, whereas AZT was more potent in PHA-PBM than in R-PBM and ddI was more potent in R-PBM. These data suggest a potential clinical application of KNI-272 and its analogs.

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页码：25 / 38

页数：14

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