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Synthesis and Evaluation of Homoazasugars as Glycosidase Inhibitors
Wong, Chi-Huey,Louis, Provencher,John A. Porco, Jr.,Jung, Sang-Hun,Wang, Yi-Fong,Chen, Lihren,Wang, Ruo,Darryl H. Steensma 충남대학교 약학대학 의약품개발연구소 1995 藥學論文集 Vol.11 No.-
In an effort to develop transition-state mimetics of the glycosidase-catalyzed reaction, five- and six-membered azasugars and their homo-analogs were prepared and tested as inhibitors of glycosidases. Inhibition studies indicate that the fucosyl cationlike, five-membered imine 1 and its reduced form 2 are potent inhibitors of α-fucosidase from bovine kideney with respective K_i values of 160 nM and 2μM. The five-membered homoaminoazasugar 3 is also a potent inhibitor of the enzyme (K_i=1.9×10^-6M), while the glucose and mannose-like six-membered homoaminoazasugars 4 and 5 are less potent than the corresponding 1-deoxyazasugars as inhibitors of α-glucosidase and α-mannosidase, respectively. The primary amino group was placed in an attempt to introduce additional electrostatic interactions in the active site. The inhibitory activities are, however, in the high μM range. Synthesis of homoazasugars structurally related to a disaccharide and a nucleoside is also described.
Design and Synthesis of Carbohydrate-based HIV Vaccine
Chung-Yi Wu,S. Shivatare Sachin,Shiou-Ting Lee,Chi-Hui Liang,Chi-Huey Wong 한국당과학회 2012 한국당과학회 학술대회 Vol.2012 No.1
The HIV-1 envelope is a basic lipid bilayer that contains gp120 and gp41 glycoproteins. Several animal models studies have demonstrated that antibodies can provide considerable benefit against HIV or SIV (Simian Immunodeficiency Virus) challenge and prompted an interest in inducing broadly neutralizing antibodies, an ultimate goal in HIV vaccine research. However, the HIV vaccine development has been deterred by the low antigenicity and immunogenicity of the HIV envelope glycoprotein gp120 and the efficient hiding of highly immunogenic epitopes by their surface glycans. Recently, a new class of bNABs (PG9, PG16, PGT121-137, and PGT141-145) isolated from HIV positive donors was shown to be potent in neutralizing primary HIV-1 strains across clades. Here we describe our efforts towards chemical and enzymatic synthesis of various gp-120 related high-mannose, hybrid, and complex type N-Glycans. We studied specificities of various bNABs towards synthetic N-glycans printed on glass slides using carbohydrate microarray. Based on recognition patterns of bNABs to quaternary structure at variable domain (V1/V2 and V3 regions) of gp-120, we created synthetic oligomannose constructs that more effectively mimic the glycan display found on gp120 and further optimized strategies to conjugate these constructs to carrier protein molecule.