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 journalArticlepeer-review

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 languageEnglish
JournalRSC Chemical Biology
Early online date27 Nov 2020
DOIs
Publication statusE-pub ahead of print - 27 Nov 2020

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