Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Wertheim cung cấp cho các bạn kiến thức về ngành y đề tài: Inhibition of human immunodeficiency virus type-1 by cdk inhibitors. | Guendel et al. AIDS Research and Therapy 2010 7 7 http content 7 1 7 AIDS RESEARCH AND THERAPY RESEARCH Open Access Inhibition of human immunodeficiency virus type-1 by cdk inhibitors I z zz zz zz I I zz zz I 1 3 h c z-zz z zz z zz I I I I A zz r-zzz 1 l-z 2 h 1 . I zz zz zz IC zz I Z zz I_I -z I 13 c z l-z I - r c zz zk 1133 Irene Guendel Emmanuel I AyDOnan Kyiene Kenn-naii Fatah Kasnancni Abstract Current therapy for human immunodeficiency virus HIV-1 infection relies primarily on the administration of antiretroviral nucleoside analogues either alone or in combination with HIV-protease inhibitors. Although these drugs have a clinical benefit continuous therapy with the drugs leads to drug-resistant strains of the virus. Recently significant progress has been made towards the development of natural and synthetic agents that can directly inhibit HIV-1 replication or its essential enzymes. We previously reported on the pharmacological cyclin-dependent kinase inhibitor PCI r-roscovitine as a potential inhibitor of HIV-1 replication. PCIs are among the most promising novel antiviral agents to emerge over the past few years. Potent activity on viral replication combined with proliferation inhibition without the emergence of resistant viruses which are normally observed in HAART patients make PCIs ideal candidates for HIV-1 inhibition. To this end we evaluated twenty four cdk inhibitors for their effect on HIV-1 replication in vitro. Screening of these compounds identified alsterpaullone as the most potent inhibitor of HIV-1 with activity at 150 nM. We found that alsterpaullone effectively inhibits cdk2 activity in HIV-1 infected cells with a low IC50 compared to control uninfected cells. The effects of alsterpaullone were associated with suppression of cdk2 and cyclin expression. Combining both alsterpaullone and r-roscovitine cyc202 in treatment exhibited even stronger inhibitory activities in HIV-1 infected PBMCs. Background Human .
