Potent and selective photo-inactivation of proteins with peptoid-ruthenium conjugates
SCIE
SCOPUS
- Title
- Potent and selective photo-inactivation of proteins with peptoid-ruthenium conjugates
- Authors
- Lee, JY; Udugamasooriya, DG; Lim, HS; Kodadek, T
- Date Issued
- 2010-04
- Publisher
- Nature Publishing Group
- Abstract
- 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.
- Keywords
- PROTEASOME REGULATORY PARTICLE; ASSISTED LIGHT INACTIVATION; LASER INACTIVATION; MOLECULAR-OXYGEN; 20S PROTEASOME; INHIBITOR; IDENTIFICATION; PHARMACOPHORE; COMPLEXES; ATPASES
- URI
- https://oasis.postech.ac.kr/handle/2014.oak/16855
- DOI
- 10.1038/NCHEMBIO.333
- ISSN
- 1552-4450
- Article Type
- Article
- Citation
- NATURE CHEMICAL BIOLOGY, vol. 6, no. 4, page. 258 - 260, 2010-04
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