Reactive fragments targeting carboxylate residues employing direct to biology, high-throughput chemistry
Ross P. Thomas, Emma K. Grant, Eleanor R. Dickinson, Francesca Zappacosta, Lee J. Edwards, Michael M. Hann, David House, Nicholas C. O. Tomkinson, Jacob T. Bush
Abstract
We present a carboxylate-targeting reactive fragment screening platform using 2-aryl-5-carboxytetrazole (ACT) as the photoreactive functionality. This work will provide a simple accessible method to rapidly discover tool molecules to interrogate important biological targets.
Topics & Concepts
ChemistryChemical biologyStructural biologyCarboxylateThroughputComputational biologyNanotechnologyCombinatorial chemistryBiochemistryBiologyComputer scienceMaterials scienceWirelessTelecommunicationsClick Chemistry and ApplicationsProtein Degradation and InhibitorsUbiquitin and proteasome pathways