Harnessing natural-product-inspired combinatorial chemistry and computation-guided synthesis to develop N -glycan modulators as anticancer agents

• Published in: Chemical science (Cambridge) Vol. 13; no. 21; pp. 6233 - 6243
• Main Authors: Chen, Wei-An, Chen, Yu-Hsin, Hsieh, Chiao-Yun, Hung, Pi-Fang, Chen, Chiao-Wen, Chen, Chien-Hung, Lin, Jung-Lee, Cheng, Ting-Jen R., Hsu, Tsui-Ling, Wu, Ying-Ta, Shen, Chia-Ning, Cheng, Wei-Chieh
• Format: Journal Article
• Language: English
• Published: CAMBRIDGE Royal Soc Chemistry 01.06.2022; Royal Society of Chemistry; The Royal Society of Chemistry
• Subjects: Anticancer properties; Cancer; Chemical synthesis; Chemistry; Chemistry, Multidisciplinary; Combinatorial analysis; Combinatorial chemistry; Computation; Glycan; In vivo methods and tests; Inhibitors; Modulation; Modulators; Natural products; Physical Sciences; Science & Technology; Selectivity; 5-SUBSTITUTED SWAINSONINE ANALOGS; SELECTIVE INHIBITORS; MECHANISMS; GLYCOSYLATION; SCAFFOLDS; ALPHA-MANNOSIDASE-II; CANCER

Modulation of N -glycosylation using human Golgi α-mannosidase II (α-hGMII) inhibitors is a potential anticancer approach, but the clinical utility of current α-hGMII inhibitors is limited by their co-inhibition of human lysosomal α-mannosidase (α-hLM), resulting in abnormal storage of oligomannoses...