title: Target identification of natural products and bioactive compounds using affinity-based probes.
abstract: Covering: 2010 to 2014.Advances in isolation, synthesis and screening strategies have made many bioactive substances available. However, in most cases their putative biological targets remain unknown. Herein, we highlight recent advances in target identification of natural products and bioactive compounds by using affinity-based probes. Aided by photoaffinity labelling, this strategy can capture potential cellular targets (on and off) of a natural product or bioactive compound in live cells directly, even when the compound-target interaction is reversible with moderate affinity. The knowledge of these targets may help uncover molecular pathways and new therapeutics for currently untreatable diseases. In this highlight, we will introduce the development of various photoactivatable groups, their synthesis and applications in target identification of natural products and bioactive compounds, with a focus on work done in recent years and from our laboratory. We will further discuss the strengths and weaknesses of each group and the outlooks for this novel proteome-wide profiling strategy.
authors.affiliation: Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.
authors.forename: Sijun
authors.initials: S
authors.lastname: Pan
authors.affiliation: Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.
authors.forename: Hailong
authors.initials: H
authors.lastname: Zhang
authors.affiliation: Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.
authors.forename: Chenyu
authors.initials: C
authors.lastname: Wang
authors.affiliation: Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.
authors.forename: Samantha C L
authors.initials: SC
authors.lastname: Yao
authors.affiliation: Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.
authors.forename: Shao Q
authors.initials: SQ
authors.lastname: Yao
mesh_terms: D001688:Biological Products / Q000138:chemical synthesis / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D040901:Proteomics
chemical_list: D001688:Biological Products