Fluorescent nanoparticles consisting of lipopeptides and fluorescein-modified polyanions for monitoring of protein kinase activity

Haruka Koga, Riki Toita, Takeshi Mori, Tetsuro Tomiyama, Jeong Hun Kang, Takuro Niidome, Yoshiki Katayama

研究成果: ジャーナルへの寄稿記事

15 引用 (Scopus)

抄録

Protein kinase (PK)-responsive nanoparticles (NPs) comprising a hydrophobically modified peptide substrate for PKs and a fluorescein-labeled polyanion (pA-F) were reported for monitoring PK activity via fluorescence intensity measurements. In this system, the formation of NPs by mixing lipopeptides and pA-Fs results in fluorescence quenching, while the quenched fluorescence recovered following dissociation of the NPs owing to the phosphorylation reaction of PKs. Eleven lipopeptides with different hydrophobic moieties (hydrocarbon and lithocholic acid) and four pA-Fs having main chains with differing flexibilities and fluorescein contents were synthesized and used to fabricate a series of twenty-four PK-responsive NP probes. The responses of the PK-responsive NP probes to PKs were evaluated to screen the most suitable NP probes. The assay system was then used to determine the IC 50 values for five inhibitors, the results of which were very similar to those previously reported. Thus, PK-responsive NPs are useful tools for high-throughput screening (HTS) of PK inhibitors.

元の言語英語
ページ(範囲)1526-1534
ページ数9
ジャーナルBioconjugate Chemistry
22
発行部数8
DOI
出版物ステータス出版済み - 8 17 2011

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Lipopeptides
Fluorescein
Nanoparticles
Protein Kinases
Proteins
Monitoring
Fluorescence
Lithocholic Acid
Phosphorylation
Protein Kinase Inhibitors
Hydrocarbons
polyanions
Peptides
Quenching
Assays
Screening
Throughput
Acids
Substrates

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Bioengineering
  • Biomedical Engineering
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry

これを引用

Fluorescent nanoparticles consisting of lipopeptides and fluorescein-modified polyanions for monitoring of protein kinase activity. / Koga, Haruka; Toita, Riki; Mori, Takeshi; Tomiyama, Tetsuro; Kang, Jeong Hun; Niidome, Takuro; Katayama, Yoshiki.

:: Bioconjugate Chemistry, 巻 22, 番号 8, 17.08.2011, p. 1526-1534.

研究成果: ジャーナルへの寄稿記事

Koga, Haruka ; Toita, Riki ; Mori, Takeshi ; Tomiyama, Tetsuro ; Kang, Jeong Hun ; Niidome, Takuro ; Katayama, Yoshiki. / Fluorescent nanoparticles consisting of lipopeptides and fluorescein-modified polyanions for monitoring of protein kinase activity. :: Bioconjugate Chemistry. 2011 ; 巻 22, 番号 8. pp. 1526-1534.
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abstract = "Protein kinase (PK)-responsive nanoparticles (NPs) comprising a hydrophobically modified peptide substrate for PKs and a fluorescein-labeled polyanion (pA-F) were reported for monitoring PK activity via fluorescence intensity measurements. In this system, the formation of NPs by mixing lipopeptides and pA-Fs results in fluorescence quenching, while the quenched fluorescence recovered following dissociation of the NPs owing to the phosphorylation reaction of PKs. Eleven lipopeptides with different hydrophobic moieties (hydrocarbon and lithocholic acid) and four pA-Fs having main chains with differing flexibilities and fluorescein contents were synthesized and used to fabricate a series of twenty-four PK-responsive NP probes. The responses of the PK-responsive NP probes to PKs were evaluated to screen the most suitable NP probes. The assay system was then used to determine the IC 50 values for five inhibitors, the results of which were very similar to those previously reported. Thus, PK-responsive NPs are useful tools for high-throughput screening (HTS) of PK inhibitors.",
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AU - Mori, Takeshi

AU - Tomiyama, Tetsuro

AU - Kang, Jeong Hun

AU - Niidome, Takuro

AU - Katayama, Yoshiki

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