Fluorometric assay of integrin activity with a small-molecular probe that senses the binding site microenvironment

Toru Komatsu; Aoi Takeda; Kenjiro Hanaoka; Takuya Terai; Tasuku Ueno; Yukio Tada; Tetsuo Nagano; Yasuteru Urano

doi:10.1039/c4cc05591h

Fluorometric assay of integrin activity with a small-molecular probe that senses the binding site microenvironment

Toru Komatsu, Aoi Takeda, Kenjiro Hanaoka, Takuya Terai, Tasuku Ueno, Yukio Tada, Tetsuo Nagano, Yasuteru Urano

Research output: Contribution to journal › Article › peer-review

3 Citations (Scopus)

Abstract

We have developed a small-molecular probe, consisting of cyclic RGD pentapeptides bearing a nitrobenzoxadiazole fluorophore at the 4′-residue, which detects integrin α_Vβ₃ activity in terms of fluorescence intensity decrease due to quenching of the fluorophore by interaction with tyrosine-122 at the binding site of the protein. This probe appears to be suitable for a practical, high-throughput fluorescence assay to screen small-molecular modulators of integrin activity.

Original language	English
Pages (from-to)	15894-15896
Number of pages	3
Journal	Chemical Communications
Volume	50
Issue number	100
DOIs	https://doi.org/10.1039/c4cc05591h
Publication status	Published - 2014 Nov 20
Externally published	Yes

ASJC Scopus subject areas

Catalysis
Electronic, Optical and Magnetic Materials
Ceramics and Composites
Chemistry(all)
Surfaces, Coatings and Films
Metals and Alloys
Materials Chemistry

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10.1039/c4cc05591h

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abstract = "We have developed a small-molecular probe, consisting of cyclic RGD pentapeptides bearing a nitrobenzoxadiazole fluorophore at the 4′-residue, which detects integrin αVβ3 activity in terms of fluorescence intensity decrease due to quenching of the fluorophore by interaction with tyrosine-122 at the binding site of the protein. This probe appears to be suitable for a practical, high-throughput fluorescence assay to screen small-molecular modulators of integrin activity.",

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T1 - Fluorometric assay of integrin activity with a small-molecular probe that senses the binding site microenvironment

AU - Komatsu, Toru

AU - Takeda, Aoi

AU - Hanaoka, Kenjiro

AU - Terai, Takuya

AU - Ueno, Tasuku

AU - Tada, Yukio

AU - Nagano, Tetsuo

AU - Urano, Yasuteru

PY - 2014/11/20

Y1 - 2014/11/20

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AB - We have developed a small-molecular probe, consisting of cyclic RGD pentapeptides bearing a nitrobenzoxadiazole fluorophore at the 4′-residue, which detects integrin αVβ3 activity in terms of fluorescence intensity decrease due to quenching of the fluorophore by interaction with tyrosine-122 at the binding site of the protein. This probe appears to be suitable for a practical, high-throughput fluorescence assay to screen small-molecular modulators of integrin activity.

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JO - Chemical Communications

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ER -

Fluorometric assay of integrin activity with a small-molecular probe that senses the binding site microenvironment

Abstract

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