A Click-Triggered Bioorthogonal Strategy for Dual Activation of Covalent Warheads and Reporter Payloads.
Michael acceptors are indispensable electrophilic motifs in chemical biology and covalent drug discovery, yet their intrinsic "always-on" reactivity frequently causes off-target modification and limits therapeutic precision. Here we report a bioorthogonal strategy for externally controlling Michael acceptor reactivity...