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Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.
TLDR
These results provide a basis for constructing new tools for probing the biology of GPR120 and for developing new candidate therapeutic agents. Expand
Design, synthesis, and biological activity of a novel series of human sirtuin-2-selective inhibitors.
TLDR
3'-phenethyloxy-2-anilinobenzamide derivatives represent an entry into a new class of SIRT2-selective inhibitors, and induced a dose-dependent selective increase of α-tubulin acetylation in human colon cancer HCT116 cells, indicating selective inhibition of Sirtuin 2 in the cells. Expand
Key bioactive reaction products of the NO/H2S interaction are S/N-hybrid species, polysulfides, and nitroxyl
TLDR
The results unveil an unexpectedly rich network of coupled chemical reactions between NO and H2S/sulfide, suggesting that the bioactivity of either transmitter is governed by concomitant formation of polysulfides and anionic S/N-hybrid species. Expand
Identification of cell-active lysine specific demethylase 1-selective inhibitors.
TLDR
The first small-molecule LSD1-selective inhibitors are identified and show in vivo H3K4-methylating activity and antiproliferative activity and should be useful as lead structures for anticancer drugs and as tools for studying the biological roles of LSD1. Expand
Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate.
TLDR
Thiolate analogues designed based on the structure of an HDAC6-selective substrate and evaluated the histone/alpha-tubulin acetylation selectivity by Western blot analysis found novel histone deacetylase 6 (HDAC6)-selective inhibitors. Expand
Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors.
TLDR
Findings suggest that combination treatment with JMJD2 inhibitors and LSD1 inhibitors may represent a novel strategy for anticancer chemotherapy. Expand
Identification of Highly Selective and Potent Histone Deacetylase 3 Inhibitors Using Click Chemistry-Based Combinatorial Fragment Assembly
TLDR
These findings indicate that HDAC3-selective inhibitors are promising candidates for anticancer drugs and antiviral agents and suggest the usefulness of the click chemistry approach to find isozyme- selective HDAC inhibitors. Expand
Photoinduced nitric oxide release from a hindered nitrobenzene derivative by two-photon excitation.
TLDR
This is the first account of a non-nitrosyl-chelated metal ion containing NO donor which can be controlled by the TPE technique. Expand
Profiling and relative quantification of multiply nitrated and oxidized fatty acids
TLDR
In vitro nitration was successfully used to establish a targeted LC–MS/MS method that was applied to complex biological samples for quantifying diverse NO2-FA and confirmed the presence of multiply nitrated and nitro-oxidized fatty acids in biological systems for the first time. Expand
Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.
TLDR
It is suggested that HDAC6-selective inhibitors have potential as anticancer agents because of the presence of a bulky alkyl group and tert-butylcarbamate group in these compounds. Expand
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