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

Jiyong Lee, D. Gomika Udugamasooriya, Hyun-Suk Lim, Thomas Kodadek

Research output: Contribution to journalArticle

53 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)258-260
Number of pages3
JournalNature Chemical Biology
Volume6
Issue number4
DOIs
StatePublished - Apr 2010

Fingerprint

Peptoids
Singlet Oxygen
Photosensitizing Agents
Ruthenium
Protein Binding
Light
Proteins
tris(2,2'-bipyridine)ruthenium II

ASJC Scopus subject areas

  • Cell Biology
  • Molecular Biology

Cite this

Potent and selective photo-inactivation of proteins with peptoid-ruthenium conjugates. / Lee, Jiyong; Udugamasooriya, D. Gomika; Lim, Hyun-Suk; Kodadek, Thomas.

In: Nature Chemical Biology, Vol. 6, No. 4, 04.2010, p. 258-260.

Research output: Contribution to journalArticle

Lee, Jiyong ; Udugamasooriya, D. Gomika ; Lim, Hyun-Suk ; Kodadek, Thomas. / Potent and selective photo-inactivation of proteins with peptoid-ruthenium conjugates. In: Nature Chemical Biology. 2010 ; Vol. 6, No. 4. pp. 258-260.
@article{55c794e933b04fe7b40b895f4d00681a,
title = "Potent and selective photo-inactivation of proteins with peptoid-ruthenium conjugates",
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.",
author = "Jiyong Lee and Udugamasooriya, {D. Gomika} and Hyun-Suk Lim and Thomas Kodadek",
year = "2010",
month = "4",
doi = "10.1038/nchembio.333",
language = "English",
volume = "6",
pages = "258--260",
journal = "Nature Chemical Biology",
issn = "1552-4450",
publisher = "Nature Publishing Group",
number = "4",

}

TY - JOUR

T1 - Potent and selective photo-inactivation of proteins with peptoid-ruthenium conjugates

AU - Lee, Jiyong

AU - Udugamasooriya, D. Gomika

AU - Lim, Hyun-Suk

AU - Kodadek, Thomas

PY - 2010/4

Y1 - 2010/4

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=77949874846&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=77949874846&partnerID=8YFLogxK

U2 - 10.1038/nchembio.333

DO - 10.1038/nchembio.333

M3 - Article

C2 - 20228793

AN - SCOPUS:77949874846

VL - 6

SP - 258

EP - 260

JO - Nature Chemical Biology

JF - Nature Chemical Biology

SN - 1552-4450

IS - 4

ER -