Target Identification of a 1,3,4-Oxadiazin-5(6H)-One Anticancer Agent via Photoaffinity Labelling

Abstract

Photoaffinity labelling probes, OPALs, were rationally designed and synthesized to identify interacting protein targets of 1,3,4-oxadiazin-5(6H)-one (LL-2003). The labelling strategy enabled successful photo-crosslinking with target proteins in both insect cell lysates and mammalian live cells, demonstrating the efficient and selective labelling of Src. A LC-MS/MS analysis of the IGF-1R overexpressed insect proteome labelled by OPALs identified the binding location of the synthesized probes. More information can be found in the Communication by Jeeyeon Lee et al.