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Bioorganic Chemistry(Chemistry)

Yamaguchi TakaoAssociate professor / Lecturer

I received my PhD in 2008 from the Graduate School of Pharmaceutical Sciences, Osaka University, and I moved to University of Notre Dame and got started the research on inhibitors of bacterial cell-wall recycling. In 2010, I started chemical biology research focused on the mechanism of a novel type of cell-death inhibitor at RIKEN. Then, I came back to Osaka University in 2013 and have developed novel artificial nucleic acid for use in therapeutic oligonucleotides. I moved to The University of Tokyo as an Assistant Professor in 2014 and have developed several bioactive small molecules and target protein identification methods. From 2017, I have been an Associate Professor at Osaka University.

Research theme

Development of artificial nucleic acids for therapeutic oligonucleotides

Therapeutic oligonucleotides are novel modality that can target DNA and RNA, and have been attracting attention in recent years. We conduct a series of drug discovery (design, synthesis, and biophysical and biological evaluations) based on the development of novel artificial nucleic acids.

Labeling and chemical modification of proteins

Target identification is important step for understanding the mechanism of bioactive small molecules. We have been developing affinity labeling methods that can be used for a specific labeling of the target protein of bioactive small molecules even in living cells. We also develop chemical modification methods for peptides and proteins.

Representative achievements

Synthesis and duplex-forming ability of oligonucleotides modified with 4′-C,5′-C-methylene-bridged nucleic acid (4′,5′-BNA). Bioorg. Med. Chem. 2021, 46, 116359.

Synthesis and properties of oligonucleotides having ethynylphosphonate (EP) linkages. J. Org. Chem. 2020, 85, 1794–1801.

Detection of esterase activity by chromogenic and fluorogenic probe based on an O-nitrobenzoxadiazole (O-NBD) unit. Bioorg. Med. Chem. 2019, 27, 1444–1448.

Hybridization and mismatch discrimination abilities of 2′,4′-bridged nucleic acids bearing 2-thiothymine or 2-selenothymine nucleobase. J. Org. Chem. 2019, 84, 1430–1439.

Specific fluorescence labeling of target proteins by using a ligand–4-azidophthalimide conjugate. Chem. Commun. 2017, 53, 8751–8754.

Synthesis of scpBNA-mC, -A and -G monomers and evaluation of the binding affinities of scpBNA-modified oligonucleotides toward complementary ssRNA and ssDNA. J. Org. Chem. 2016, 81, 11000–11008.

Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor / (PPAR/) dual agonists. Bioorg. Med. Chem. 2016, 24, 5455–5461.

Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptor / (PPAR/) dual agonistic activity. Bioorg. Med. Chem. 2016, 24, 5258–5269.

Synthesis and properties of 2′-O,4′-C-spirocyclopropylene bridged nucleic acid (scpBNA), an analogue of 2′,4′-BNA/LNA bearing a cyclopropane ring. Chem. Commun. 2015, 51, 9737–9740.

Turn-ON fluorescent affinity labeling using a small bifunctional O-nitrobenzoxadiazole unit. Chem. Sci. 2014, 5, 1021–1029.