title: Advances in identification and validation of protein targets of natural products without chemical modification.
abstract: Covering: up to February 2016Identification of the target proteins of natural products is pivotal to understanding the mechanisms of action to develop natural products for use as molecular probes and potential therapeutic drugs. Affinity chromatography of immobilized natural products has been conventionally used to identify target proteins, and has yielded good results. However, this method has limitations, in that labeling or tagging for immobilization and affinity purification often result in reduced or altered activity of the natural product. New strategies have recently been developed and applied to identify the target proteins of natural products and synthetic small molecules without chemical modification of the natural product. These direct and indirect methods for target identification of label-free natural products include drug affinity responsive target stability (DARTS), stability of proteins from rates of oxidation (SPROX), cellular thermal shift assay (CETSA), thermal proteome profiling (TPP), and bioinformatics-based analysis of connectivity. This review focuses on and reports case studies of the latest advances in target protein identification methods for label-free natural products. The integration of newly developed technologies will provide new insights and highlight the value of natural products for use as biological probes and new drug candidates.
authors.affiliation: Department of Biotechnology, Translational Research Center for Protein Function Control, College of Life Science & Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea. kwonhj@yonsei.ac.kr.
authors.forename: J
authors.initials: J
authors.lastname: Chang
authors.affiliation: Department of Biotechnology, Translational Research Center for Protein Function Control, College of Life Science & Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea. kwonhj@yonsei.ac.kr.
authors.forename: Y
authors.initials: Y
authors.lastname: Kim
authors.affiliation: Department of Biotechnology, Translational Research Center for Protein Function Control, College of Life Science & Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea. kwonhj@yonsei.ac.kr and Department of Internal Medicine, Yonsei University College of Medicine, Seoul 120-752, Republic of Korea.
authors.forename: H J
authors.initials: HJ
authors.lastname: Kwon
mesh_terms: D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology; D016503:Drug Delivery Systems; D055808:Drug Discovery; D015394:Molecular Structure; D011506:Proteins / Q000378:metabolism*; D040901:Proteomics; D054852:Small Molecule Libraries
chemical_list: D001688:Biological Products; D011506:Proteins; D054852:Small Molecule Libraries