title: A bioorthogonal approach for imaging the binding between Dasatinib and its target proteins inside living cells.
abstract: Herein, we present a simple readout of the binding between a chemical drug and its target proteins in the cytoplasm by using a two-step bioorthogonal labeling method combined with spatially-localized expression of proteins. Dasatinib was modified with trans-cyclooctene (TCO), and its cytoplasmic target kinases were expressed in intracellular compartments, such as endosomes and F-actins. After bioorthogonal labeling, the colocalization between Dasatinib and its target proteins was observed in intracellular compartments.
authors.affiliation: Division of Bioconvergence Analysis, Korea Basic Science Institute (KBSI), Daejeon 34133, Korea. kblee@kbsi.re.kr.
authors.forename: Young-Rang
authors.initials: YR
authors.lastname: Kim
authors.affiliation: Biomedical Omics Group, Korea Basic Science Institute (KBSI), Cheongju 28119, Korea.
authors.forename: Young Hye
authors.initials: YH
authors.lastname: Kim
authors.affiliation: Division of Bioconvergence Analysis, Korea Basic Science Institute (KBSI), Daejeon 34133, Korea. kblee@kbsi.re.kr.
authors.forename: Sung Woo
authors.initials: SW
authors.lastname: Kim
authors.affiliation: Division of Bioconvergence Analysis, Korea Basic Science Institute (KBSI), Daejeon 34133, Korea. kblee@kbsi.re.kr.
authors.forename: Yong Ju
authors.initials: YJ
authors.lastname: Lee
authors.affiliation: Division of Bioconvergence Analysis, Korea Basic Science Institute (KBSI), Daejeon 34133, Korea. kblee@kbsi.re.kr and Graduate School of Analytical Science and Technology (GRAST), Chungnam National University, Daejeon 34134, Korea.
authors.forename: Dong-Eon
authors.initials: DE
authors.lastname: Chae
authors.affiliation: Division of Bioconvergence Analysis, Korea Basic Science Institute (KBSI), Daejeon 34133, Korea. kblee@kbsi.re.kr and Graduate School of Analytical Science and Technology (GRAST), Chungnam National University, Daejeon 34134, Korea.
authors.forename: Kyung-A
authors.initials: KA
authors.lastname: Kim
authors.affiliation: Drug Discovery System & Pharmaceuticals, Inc. (DDSPharm), Daejeon 34165, Korea.
authors.forename: Zee-Won
authors.initials: ZW
authors.lastname: Lee
authors.affiliation: New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Daegu 41061, Korea.
authors.forename: Nam Doo
authors.initials: ND
authors.lastname: Kim
authors.affiliation: Division of Bioconvergence Analysis, Korea Basic Science Institute (KBSI), Daejeon 34133, Korea. kblee@kbsi.re.kr and Graduate School of Analytical Science and Technology (GRAST), Chungnam National University, Daejeon 34134, Korea.
authors.forename: Jong-Soon
authors.initials: JS
authors.lastname: Choi
authors.affiliation: Center for Cell-Encapsulation Research and Department of Chemistry, Korea Advanced Institute of Science and Technology (KAIST), Daejeon 34141, Korea. ischoi@kaist.ac.kr.
authors.forename: Insung S
authors.initials: IS
authors.lastname: Choi
authors.affiliation: Division of Bioconvergence Analysis, Korea Basic Science Institute (KBSI), Daejeon 34133, Korea. kblee@kbsi.re.kr.
authors.forename: Kyung-Bok
authors.initials: KB
authors.lastname: Lee
mesh_terms: D000199:Actins / Q000737:chemistry / Q000378:metabolism*; D000081247:CSK Tyrosine-Protein Kinase; D034242:Cyclooctanes / Q000737:chemistry; D003593:Cytoplasm / Q000378:metabolism; D000069439:Dasatinib / Q000737:chemistry / Q000378:metabolism*; D011992:Endosomes / Q000378:metabolism; D006367:HeLa Cells; D006801:Humans; D008856:Microscopy, Fluorescence; D011485:Protein Binding; D011494:Protein Kinases / Q000737:chemistry / Q000378:metabolism*; D019061:src-Family Kinases / Q000737:chemistry / Q000378:metabolism
chemical_list: D000199:Actins; D034242:Cyclooctanes; D011494:Protein Kinases; D000081247:CSK Tyrosine-Protein Kinase; D019061:src-Family Kinases; C000631346:CSK protein, human; D000069439:Dasatinib