Covalent Proximity Scanning of a Distal Cysteine to Target PI3Kα
Chiara Borsari, Erhan Keleş, Jacob A. McPhail, Alexander Schaefer, Rohitha Sriramaratnam, Wojciech Goch, Thorsten Schaefer, Martina De Pascale, Wojciech Bal, Matthias Gstaiger, John E. Burke, Matthias P. Wymann
Abstract
thus qualify as specific chemical probes to explore PI3Kα-selective signaling branches. The proposed approach is generally suited to develop covalent tools targeting distal, unexplored Cys residues in biologically active enzymes.
Topics & Concepts
ChemistryCovalent bondLinkerCysteineElectrophileSmall moleculeBiophysicsCombinatorial chemistryBioorthogonal chemistryBiochemistryStereochemistryEnzymeClick chemistryOrganic chemistryBiologyCatalysisComputer scienceOperating systemClick Chemistry and ApplicationsProtein Degradation and InhibitorsChemical Synthesis and Analysis