Asset Details
Do you wish to reserve the book?
Bright and stable luminescent probes for target engagement profiling in live cells
Hey, we have placed the reservation for you!
By the way, why not check out events that you can attend while you pick your title.
Oops! Something went wrong.
Looks like we were not able to place the reservation. Kindly try again later.
Are you sure you want to remove the book from the shelf?
Bright and stable luminescent probes for target engagement profiling in live cells
Do you wish to request the book?
Bright and stable luminescent probes for target engagement profiling in live cells
Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy
We have requested the book for you!
Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.
Oops! Something went wrong.
Looks like we were not able to place your request. Kindly try again later.
Journal Article
Bright and stable luminescent probes for target engagement profiling in live cells
2021
Overview
The pace of progress in biomedical research directly depends on techniques that enable the quantitative interrogation of interactions between proteins and other biopolymers, or with their small-molecule ligands. Time-resolved Förster resonance energy transfer (TR-FRET) assay platforms offer high sensitivity and specificity. However, the paucity of accessible and biocompatible luminescent lanthanide complexes, which are essential reagents for TR-FRET-based approaches, and their poor cellular permeability have limited broader adaptation of TR-FRET beyond homogeneous and extracellular assay applications. Here, we report the development of CoraFluors, a new class of macrotricyclic terbium complexes, which are synthetically readily accessible, stable in biological media and exhibit photophysical and physicochemical properties that are desirable for biological studies. We validate the performance of CoraFluors in cell-free systems, identify cell-permeable analogs and demonstrate their utility in the quantitative domain-selective characterization of Keap1 ligands, as well as in isoform-selective target engagement profiling of HDAC1 inhibitors in live cells.
CoraFluors, a class of macrocyclic terbium complexes for use in time-resolved FRET, exhibit physicochemical properties desirable for biological studies, including characterization of Keap1 ligands and HDAC1 target engagement profiling in live cells.
Publisher
Nature Publishing Group US,Nature Publishing Group
Subject
/ Chemistry and Materials Science
/ Coordination Complexes - chemical synthesis
/ Coordination Complexes - chemistry
/ Coordination Complexes - pharmacology
/ Fluorescence Resonance Energy Transfer
/ Fluorescent Dyes - chemical synthesis
/ Fluorescent Dyes - chemistry
/ Fluorescent Dyes - pharmacology
/ Humans
/ Kelch-Like ECH-Associated Protein 1 - antagonists & inhibitors
/ Kelch-Like ECH-Associated Protein 1 - metabolism
/ Ligands
/ Reagents
/ Terbium
