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Chem Commun (Camb). 2016 Sep 27;52(79):11764-11767.

A bioorthogonal approach for imaging the binding between Dasatinib and its target proteins inside living cells.

Author information

1
Division of Bioconvergence Analysis, Korea Basic Science Institute (KBSI), Daejeon 34133, Korea. kblee@kbsi.re.kr.
2
Biomedical Omics Group, Korea Basic Science Institute (KBSI), Cheongju 28119, Korea.
3
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.
4
Drug Discovery System & Pharmaceuticals, Inc. (DDSPharm), Daejeon 34165, Korea.
5
New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Daegu 41061, Korea.
6
Center for Cell-Encapsulation Research and Department of Chemistry, Korea Advanced Institute of Science and Technology (KAIST), Daejeon 34141, Korea. ischoi@kaist.ac.kr.

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.

PMID:
27711355
DOI:
10.1039/c6cc07011f
[Indexed for MEDLINE]

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