KATO Atsushi

J-GLOBAL         Last updated: Apr 1, 2019 at 15:23
KATO Atsushi
University of Toyama
Hospital, Department of Pharmacy
Job title
Associate Professor and Vice Director
Research funding number


【Examples of current projects】

1) Iminosugars as potential therapeutic agents

Glycosidases are involved in several important anabolic and catabolic process, such as intestinal digestion, lysosomal catabolism, and post-translational modification, which are closely related to the endoplasmic reticulum (ER) quality control and ER-associated degradation of glycoproteins. Thus, glycosidase-inhibiting iminosugars could have enormous potential applications as biochemical tools and therapeutic agents. These iminosugars can inhibit various glycosidases because of a structural resemblance to their sugar moiety to natural substrates. For example, N-hydroxyetheyl-1-deoxynojirimycin (GlysetTM), which corresponds to an α-D-glucose configuration, has been approved as a second-generation α-glucosidase inhibitor to treat type-2 diabetes. N-Butyl-1-deoxynojirimycin (ZavescaTM) is an inhibitor of ceramide-specific glucosyltransferase and has been approved for the oral treatment of substrate reduction therapy in type-1 Gaucher disease. The iminosugar derivatives, α-6-C-nonylisofagomine, α-1-C-nonyl-1,5-dodeoxy-1,5-iminoxylitol, and α-1-C-octyl-1-deoxynojirimycin are candidates as oral agents of pharmacological chaperone therapy in type-1 Gaucher disease. Our laboratory provides a unique opportunity to find a range of new medicines for different therapeutic areas from compounds of a defined chemical class.

2) Isolation of water-soluble bioactive components from medicinal plants

Herbal medicines were often traditionally prepared in water but active compounds soluble in water are often hidden by high concentrations of primary metabolites. Our laboratory has a unique experience and track record in identifying novel bioactive compounds in plant water-soluble fractions that can often fully explain the claimed activities of the plants. We believe that the elusive active components of many herbal medicines reside in the water-soluble extractable material; the failure to understand these components may well explain the variable results obtained for many herbal preparations. The water-soluble components of many food plants and products have also been found by our research to contain novel functional components.

Research Areas


Awards & Honors

Tetrahedron: Asymmetry Most Cited Paper 2004-2007 Award (Elsevier)
Bioorganic & Medicinal Chemistry: Most Cited Paper 2006-2009 Award (Elsevier)
The Journal of Agricultural and Food Chemistry: Most active reviewers 2008-2009 Award (The American Chemical Society)
Tetrahedron: Asymmetry: Top-25 Most Cited Articles 2010-2011 Award (Elsevier)

Published Papers

J. Nat. Prod.   82(2) 358-367   2019   [Refereed]
Chem Biol Drug Des.   92(1) 1171-1197   2018   [Refereed]
J. Org. Chem.   83(10) 5558-5576   2018   [Refereed]
Chin. Chem. Lett.   28(8) 1701-1704   2017   [Refereed]
Chem. Eur. J.   23(38) 9022-9025   2017   [Refereed]


Takahata Hiroki, Ouchi Hidekazu, Banba Yasunori, Kato Atsushi, Adachi Isao, Asano Naoki
天然有機化合物討論会講演要旨集   (46) 467-472   Oct 2004
Azasugars (or iminosugars) are an important class of glycosidase inhibitors and are arousing great interest as potential therapeutic agents such as antidiabetics, antiobesities, antivirals, and therapeutic agents for some genetic disorders. Miglit...
Takahata Hiroki, Mihara Yukiko, Ouchi Hidekazu, Banba Yasunori, Nemoto Hideo, Kato Atsushi, Adachi Isao
天然有機化合物討論会講演要旨集   (45) 419-424   Sep 2003
Polyhydroxylated nitrogen heterocycles azasugars may be considered to be mimics of sugars in which the ring oxygen has been substituted for a nitrogen atom. The often potent inhibitory activity of many of these compounds toward carbohydrate-proces...
Aono Shuka, Kawakami Naomi, Kato Atsushi, Kawakami Junichi, Adachi Isao
Japanese journal of pharmaceutical health care and sciences   27(2) 105-112   Apr 2001
Digoxin-like factor (DLF) is known to interfere with a digoxin assay and falsely elevate the digoxin concentration. DLF has been reported in patients with liver and renal diseases, terminal pregnant women and infants. In this study, cholestasic ra...

Books etc

Calystegine alkaloids in the potatoes and other food plants : Symposium Series No. 745/Natural and Synthetic Toxins: Biological Implications
ACS, Washington   1999   

Conference Activities & Talks

Protective effects of dietary 1,5-Anhydro-D-glucitol in diabetes and metabolic syndrome.
2015 International Chemical Congress of Pacific Basin Societies (PACIFICHEM 2015)   2015   
Catalytic asymmetric syntheses and biological evaluations of α-1-C-substituted L-iminofuranose derivatives as α-glucosidase inhibitor.
2015 International Chemical Congress of Pacific Basin Societies (PACIFICHEM 2015)   2015   
In silico study on the interaction of high affinity ligand calystegine B2 with β-glucocerebrosidase.
2015 International Chemical Congress of Pacific Basin Societies (PACIFICHEM 2015)   2015   
Rare sugars as potential inducers of the rhamnose operon: Biotechnology and chemistry in the production of 6-deoxy-hexoses and related monosaccharides.
Synthesis and interactions of rhamnose iminosugar mimics with the rhamnose operon, rhamnosidases, and rhamnose isomerase.
A nitro sugar based route to branched-chain polyhydroxylated octahydro-1H-indole-4,5,6-triols, as new potential glycosidase inhibitors
XI Jornadas de Carbohidratos (XI Carbohydrate Symposium)   2014   
Fluoro azetidines and difluoro prolines from D-glucose; Inhibition of pancreatic cancer cell growth by a fluoro azetidine
248th ACS National Meeting & Exposition   2014   
In vitro Iinvestigation of a novel iminosugar, TOP-DNJ.
The Third International Conference on Dengue and Dengue Haemorrhagic Fever (Global Dengue: Challenges and promises)   2013   
Synthesis amd biological evaluation of azetidines derivatives from carbohydrates.
26th International Carbohydrate Symposium (ICS2012)   2012   
Synthesis of glycosidase inhibitors based on bicyclic azetidines for the treatment of cancer.
26th International Carbohydrate Symposium (ICS2012)   2012   

Committee Memberships

Medical and Pharmaceutical Society for WAKAN-YAKU  Member of the Board of Councilors

Research Grants & Projects

Design, synthesis, and biological evaluation of novel class of iminosugar-based pharmacological chaperons for Gauchers disease
Japanese Society for the Promotion of Science (JSPS): Grant-in-Aid for Scientific Research (No: 23590127)
Project Year: 2011 - 2013
Characterization of glycosidase-inhibiting iminosugars and evaluation of their effect on glycoprotein biosynthesis
Japanese Society for the Promotion of Science (JSPS): Grant-in-Aid for Scientific Research (No: 22590059)
Project Year: 2010 - 2012
Development of new concept drugs against lysosome disease base on enzyme structures stabilized effects
Japanese Society for the Promotion of Science (JSPS): Grant-in-Aid for Scientific Research (No: 18790086)
Project Year: 2006 - 2008
Design of new pharmacological chaperones for lysosome disease
Japanese Society for the Promotion of Science (JSPS): Grant-in-Aid for Scientific Research (No: 16790080)
Project Year: 2004 - 2005
Iminosugar (azasugar) glycosidase inhibitor : varsatite tools for glycobiogists
International Collaboration
Study of glycolipid lysosomal storage diseases
International Collaboration
Project Year: 1997   
Characterization of glycosidase-inhibiting iminosugars and evaluation of their effect on N-linked oligosaccharide processing


WO2009/078423 : Fused tricyclic compound having aldose reductase inhibitory activity
Disclosed is a fused tricyclic compound having aldose reductase inhibitory activity. Specifically disclosed is a fused tricyclic compound represented by general formula (I). [In the formula (I), R1 represents a hydrogen atom, a halogen atom or the...
WO/2011/058975 : Agent for ameliorating postprandial hyperglycemia, and pyrrolidine iminosugar or salt thereof
Disclosed is an agent for ameliorating postprandial hyperglycemia, which contains a pyrrolidine iminosugar represented by general formula (1) or a salt thereof. (In the formula, R1 represents an alkyl group which may be substituted by a group that...
WO/2010/082661 : 1,5-AG-containing composition
Disclosed is a composition for ameliorating postcibal hyperglycemia which comprises at least one member selected from the group consisting of 1,5-D-anhydroglucitol, 1,5-D-anhydrofructose and derivatives of the same. Also disclosed is a composition...
WO/2010/106871 : Osmotic pressure-controlling agent
An osmotic pressure-controlling agent which comprises 1,5-D-anhydroglucitol represented by formula (I); and a peritoneal dialysate, an ophthalmic composition and a transfusion each containing said controlling agent. Since the aforesaid osmotic pre...