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KMID : 0624620150480020121
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BMB Reports
2015 Volume.48 No. 2 p.121 ~ p.126
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Identification of a novel type of small molecule inhibitor against HIV-1
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Kim Byung-Soo
Park Jung-Ae
Kim Min-Jung
Kim Seon-Hee
Yu Kyung-Lee
You Ji-Chang
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Abstract
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Here we report a new chemical inhibitor against HIV-1 with a novel structure and mode of action. The inhibitor, designated as A1836, inhibited HIV-1 replication and virus production with a 50% inhibitory concentration (IC50) of 2.0 μM in an MT-4 cell-based and cytopathic protection antiviral assay, while its 50% cytotoxic concentration (CC50) was much higher than 50 μM. Examination of the effect of A1836 on in vitro HIV-1 reverse transcriptase (RT) and integrase showed that neither were molecular targets of A1836. The characterization and re-infection assay of the HIV-1 virions generated in the presence of A1836 showed that the synthesis of early RT products in the cells infected with the virions was inhibited dose-dependently, due in part to abnormal protein formation within the virions, thus resulting in an impaired infectivity. These results suggest that A1836 might be a novel candidate for the development of a new type of HIV-1 inhibitor.
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KEYWORD
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HIV-1 inhibitor, Infectivity, Novel chemical structure, Reverse transcription, Viral protein processing
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