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

Abstract / Description of output

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
Journal	RSC Chemical Biology
Early online date	27 Nov 2020
DOIs	https://doi.org/10.1039/D0CB00122H
Publication status	E-pub ahead of print - 27 Nov 2020

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10.1039/D0CB00122HLicence: Creative Commons: Attribution (CC-BY)

ChapmanEtalRSCCB2020ATwoStepResinBasedApproachToRevealSurvivinSelectiveFinal published version, 3.15 MBLicence: Creative Commons: Attribution (CC-BY)

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3 Finished

Pump-Priming Translational Research Initiative
Auer, M.
MRC
1/04/09 → …
Project: Research
Molecular Mechanisms of Centromere Inheritance and Kinetochore Function
Arulanandam, J.
UK-based charities
4/01/17 → 4/10/22
Project: Research
Understanding bacterial host adaptation to combat infectious diseases
Fitzgerald, R., Auer, M. & Hume, D.
UK-based charities
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Project: Research

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@article{74a9dadbb7e149b6896e56ae61a6773b,

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",

year = "2020",

month = nov,

day = "27",

doi = "10.1039/D0CB00122H",

language = "English",

journal = "RSC Chemical Biology",

issn = "2633-0679",

publisher = "Royal Society of Chemistry",

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TY - JOUR

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 - 2020/11/27

Y1 - 2020/11/27

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.

U2 - 10.1039/D0CB00122H

DO - 10.1039/D0CB00122H

M3 - Article

SN - 2633-0679

JO - RSC Chemical Biology

JF - RSC Chemical Biology

ER -

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

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Projects

Pump-Priming Translational Research Initiative

Molecular Mechanisms of Centromere Inheritance and Kinetochore Function

Understanding bacterial host adaptation to combat infectious diseases

Cite this