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Cover Feature: Target Identification of a 1,3,4‐Oxadiazin‐5(6 H )‐One Anticancer Agent via Photoaffinity Labelling (Asian J. Org. Chem. 9/2019)
Author(s) -
Lim Bumhee,
Lee Jinah,
Kim Byungjin,
Lee Rang,
Park Jaehyun,
Oh DongChan,
Gam Jongsik,
Lee Jeeyeon
Publication year - 2019
Publication title -
asian journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.846
H-Index - 44
eISSN - 2193-5815
pISSN - 2193-5807
DOI - 10.1002/ajoc.201900506
Subject(s) - labelling , chemistry , photoaffinity labeling , affinity label , proteome , fluorescent labelling , biochemistry , combinatorial chemistry , stereochemistry , binding site , fluorescence , physics , quantum mechanics
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. on page 1626 in Issue 9, 2019 (DOI: 10.1002/ajoc.201900258).