First-in-class small molecule inhibitors of the single-strand DNA cytosine deaminase APOBEC3G.

  title={First-in-class small molecule inhibitors of the single-strand DNA cytosine deaminase APOBEC3G.},
  author={Ming Li and Shivender M. D. Shandilya and Michael A Carpenter and Anurag S. Rathore and William L. Brown and Angela L. Perkins and Daniel A Harki and Jonathan Solberg and Derek J. Hook and Krishan K. Pandey and Michael A. Parniak and Jeffrey R. Johnson and Nevan J. Krogan and Mohan Somasundaran and Akbar Ali and Celia A Schiffer and Reuben S Harris},
  journal={ACS chemical biology},
  volume={7 3},
APOBEC3G is a single-stranded DNA cytosine deaminase that comprises part of the innate immune response to viruses and transposons. Although APOBEC3G is the prototype for understanding the larger mammalian polynucleotide deaminase family, no specific chemical inhibitors exist to modulate its activity. High-throughput screening identified 34 compounds that inhibit APOBEC3G catalytic activity. Twenty of 34 small molecules contained catechol moieties, which are known to be sulfhydryl reactive… CONTINUE READING
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