- 著者
- Hiroki Hosaka Sayaka Shirai Sora Fujita Mitsuru Tashiro Takako Hirano Wataru Hakamata Toshiyuki Nishio
- 出版者
- The Japanese Society of Applied Glycoscience
- 雑誌
- Journal of Applied Glycoscience (ISSN:13447882)
- 巻号頁・発行日
- vol.67, no.4, pp.129-135, 2020-11-20 (Released:2020-11-20)
- 参考文献数
- 24
- 被引用文献数
- 1
Utilizing transglycosylation reaction catalyzed by β-N-acetylhexosaminidase of Stenotrophomonas maltophilia, β-D-fructofuranosyl-(2↔1)-α-N, N´diacetylchitobioside (GlcNAc2-Fru) was synthesized from N-acetylsucrosamine and N, N´-diacetylchitobiose (GlcNAc2), and β-D-fructofuranosyl-(2↔1)-α-N, N´, N´´-triacetylchitotrioside (GlcNAc3-Fru) was synthesized from GlcNAc2-Fru and GlcNAc2. Through purification by charcoal column chromatography, pure GlcNAc2-Fru and GlcNAc3-Fru were obtained in molar yields of 33.0 % and 11.7 % from GlcNAc2, respectively. The structures of these oligosaccharides were confirmed by comparing instrumental analysis data of fragments obtained by enzymatic hydrolysis and acid hydrolysis of them with known data of these fragments.
- 著者
- Ryosuke Koyama Wataru Hakamata Takako Hirano Toshiyuki Nishio
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- pp.c17-01009, (Released:2018-03-13)
- 参考文献数
- 29
- 被引用文献数
- 9
Three Golgi mannosidases (GMs), namely Golgi α-mannosidases IA, IB, and IC, remove mannose residues from N-glycans and regulate the quality control and transportation of nascent proteins. GM inhibitors regulate several biological events such as cell–cell communication, differentiation, and apoptosis in cancer cells. As a result, GM inhibitor-based therapies have gained significant attention for cancer treatment. However, to date, no GM inhibitor has been approved and none is in clinical development for anti-cancer treatment. Meanwhile, drug repositioning plays an important role in identifying potential inhibitors that vary in molecular structure and properties to bypass much of the early cost and time. We performed a drug repositioning screen of a compound library that included approved drugs. The estrogen receptor antagonists tamoxifen and raloxifene inhibited human GMs at the cellular level. Sulindac, a nonsteroidal anti-inflammatory drug, also inhibited GMs. Our results demonstrated the efficacy of this screening strategy and revealed lead compounds for anti-cancer drug development.