A two-step resin based approach to reveal survivin-selective fluorescent probes

Andrew J. Ambrose; Nhan T. Pham; Jared Sivinski; Larissa Guimarães; Niloufar Mollasalehi; Paula Jimenez; Maria A. Abad; A. Arockia Jeyaprakash; Steven Shave; Letícia V. Costa-Lotufo; James J. La Clair; Manfred Auer; Eli Chapman

doi:10.1039/d0cb00122h

A two-step resin based approach to reveal survivin-selective fluorescent probes

Andrew J. Ambrose, Nhan T. Pham, Jared Sivinski, Larissa Guimarães, Niloufar Mollasalehi, Paula Jimenez, Maria A. Abad, A. Arockia Jeyaprakash, Steven Shave, Letícia V. Costa-Lotufo, James J. La Clair, Manfred Auer, Eli Chapman

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

3 Scopus citations

Abstract

The identification of modulators for proteins without assayable biochemical activity remains a challenge in chemical biology. The presented approach adapts a high-throughput fluorescence binding assay and functional chromatography, two protein-resin technologies, enabling the discovery and isolation of fluorescent natural product probes that target proteins independently of biochemical function. The resulting probes also suggest targetable pockets for lead discovery. Using human survivin as a model, we demonstrate this method with the discovery of members of the prodiginine family as fluorescent probes to the cancer target survivin.

Original language	English (US)
Pages (from-to)	181-186
Number of pages	6
Journal	RSC Chemical Biology
Volume	2
Issue number	1
DOIs	https://doi.org/10.1039/d0cb00122h
State	Published - 2021

ASJC Scopus subject areas

Chemistry (miscellaneous)
Biochemistry
Molecular Biology
Biochemistry, Genetics and Molecular Biology (miscellaneous)

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10.1039/d0cb00122h

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title = "A two-step resin based approach to reveal survivin-selective fluorescent probes",

abstract = "The identification of modulators for proteins without assayable biochemical activity remains a challenge in chemical biology. The presented approach adapts a high-throughput fluorescence binding assay and functional chromatography, two protein-resin technologies, enabling the discovery and isolation of fluorescent natural product probes that target proteins independently of biochemical function. The resulting probes also suggest targetable pockets for lead discovery. Using human survivin as a model, we demonstrate this method with the discovery of members of the prodiginine family as fluorescent probes to the cancer target survivin.",

author = "Ambrose, {Andrew J.} and Pham, {Nhan T.} and Jared Sivinski and Larissa Guimar{\~a}es and Niloufar Mollasalehi and Paula Jimenez and Abad, {Maria A.} and Jeyaprakash, {A. Arockia} and Steven Shave and Costa-Lotufo, {Let{\'i}cia V.} and {La Clair}, {James J.} and Manfred Auer and Eli Chapman",

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year = "2021",

doi = "10.1039/d0cb00122h",

language = "English (US)",

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T1 - A two-step resin based approach to reveal survivin-selective fluorescent probes

AU - Ambrose, Andrew J.

AU - Pham, Nhan T.

AU - Sivinski, Jared

AU - Guimarães, Larissa

AU - Mollasalehi, Niloufar

AU - Jimenez, Paula

AU - Abad, Maria A.

AU - Jeyaprakash, A. Arockia

AU - Shave, Steven

AU - Costa-Lotufo, Letícia V.

AU - La Clair, James J.

AU - Auer, Manfred

AU - Chapman, Eli

PY - 2021

Y1 - 2021

N2 - The identification of modulators for proteins without assayable biochemical activity remains a challenge in chemical biology. The presented approach adapts a high-throughput fluorescence binding assay and functional chromatography, two protein-resin technologies, enabling the discovery and isolation of fluorescent natural product probes that target proteins independently of biochemical function. The resulting probes also suggest targetable pockets for lead discovery. Using human survivin as a model, we demonstrate this method with the discovery of members of the prodiginine family as fluorescent probes to the cancer target survivin.

AB - The identification of modulators for proteins without assayable biochemical activity remains a challenge in chemical biology. The presented approach adapts a high-throughput fluorescence binding assay and functional chromatography, two protein-resin technologies, enabling the discovery and isolation of fluorescent natural product probes that target proteins independently of biochemical function. The resulting probes also suggest targetable pockets for lead discovery. Using human survivin as a model, we demonstrate this method with the discovery of members of the prodiginine family as fluorescent probes to the cancer target survivin.

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A two-step resin based approach to reveal survivin-selective fluorescent probes

Abstract

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