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KMID : 0578320130360030212
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Molecules and Cells
2013 Volume.36 No. 3 p.212 ~ p.218
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Identification of Two HIV Inhibitors that also Inhibit Human RNaseH2
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Kim Jung-Hwan
Yoon Jae-Wan
Ju Moon-Kyeong
Lee Yun-Mi
Kim Tae-Hee
Kim Jun-Won
Peter Sommer
No Zae-Sung
Jonathan Cechetto
Han Sung-Jun
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Abstract
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A total of 140,000 compounds were screened in a target-free cell-based high throughput assay against HIV-1 infection, and a subset of 81 promising compounds was identified. Secondary screening of these 81 compounds revealed two putative human RNaseH2 inhibitors, RHI001 and RHI002, with IC50 value of 6.8 ?M and 16 ?M, respec-tively. RHI002 showed selective activity against human RNaseH2 while RHI001 inhibited HIV-RNaseH, E. coli RNaseH, and human RNaseH1 with IC50 value of 28.5 ?M, 7.9 ?M, and 31.7 ?M, respectively. Kinetic analysis revealed that both inhibitors had non-competitive inhibitor-like properties. Because RNaseH2 is involved in the etiology of Aicardi-Goutier syndrome and has been suggested as an anticancer drug target, small molecule inhibitors modulating its activity would be useful for investigating the cellular function of this molecule.
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KEYWORD
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Aicardi-Goutier syndrome, cell-based screening, HIV inhibition, human RNaseH2
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