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Potent and selective photo-inactivation of proteins with peptoid-ruthenium conjugates

  作者 LEE JIYONG; UDUGAMASOORIYA D GOMIKA; LIM HYUNSUK; KODADEK THOMAS  
  选自 期刊  NATURE CHEMICAL BIOLOGY;  卷期  2010年6-4;  页码  258-260  
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[摘要]Advances in high-throughput screening now enable the rapid discovery of bioactive small molecules, but these primary hits almost always exhibit modest potency. We report a strategy for the transformation of these hits into much more potent inhibitors without compound optimization. Appending a derivative of Ru(II)(tris-bipyridyl)(2+), an efficient photosensitizer of singlet oxygen production, to synthetic protein-binding compounds results in highly potent and specific target protein inactivation upon irradiation with visible light.

 
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