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. 2009 Oct 8;52(19):5781-4.
doi: 10.1021/jm900597q.

RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information

Thorsten A Kirschberg  1 , Mini Balakrishnan, Neil H Squires, Tiffany Barnes, Katherine M Brendza, Xiaowu Chen, Eugene J Eisenberg, Weili Jin, Nilima Kutty, Stephanie Leavitt, Albert Liclican, Qi Liu, Xiaohong Liu, John Mak, Jason K Perry, Michael Wang, William J Watkins, Eric B Lansdon
Affiliations

RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information

Thorsten A Kirschberg et al. J Med Chem. .

Abstract

Pyrimidinol carboxylic acids were designed as inhibitors of HIV-1 RNase H function. These molecules can coordinate to two divalent metal ions in the RNase H active site. Inhibition of enzymatic activity was measured in a biochemical assay, but no antiviral effect was observed. Binding was demonstrated via a solid state structure of the isolated p15-Ec domain of HIV-1 RT showing inhibitor and two Mn(II) ions bound to the RNase H active site.

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