title: Potent small molecule mouse CD22-inhibitors: exploring the interaction of the residue at C-2 of sialic acid scaffold.
abstract: Our previous study revealed that compound 1 (9-(4'-hydroxy-4-biphenyl)acetamido-9-deoxy-Neu5Gcalpha2-6GalOMP) has the most promising affinity for mCD22. Replacing the subterminal galactose residue of 1 with benzyl or biphenylmethyl as aglycone led to 38- and 20-fold higher potency, respectively. This discovery represents a new direction in inhibitor design suitable for pharmaceutical development.
authors.affiliation: Department of Applied Bio-organic Chemistry, The United Graduate School of Agricultural Sciences, Gifu University, Gifu 501-1193, Japan. moazhajjaj@yahoo.com
authors.forename: Hajjaj H M
authors.initials: HH
authors.lastname: Abdu-Allah
authors.forename: Kozo
authors.initials: K
authors.lastname: Watanabe
authors.forename: Koji
authors.initials: K
authors.lastname: Hayashizaki
authors.forename: Chiaki
authors.initials: C
authors.lastname: Takaku
authors.forename: Taichi
authors.initials: T
authors.lastname: Tamanaka
authors.forename: Hiromu
authors.initials: H
authors.lastname: Takematsu
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Kozutsumi
authors.forename: Takeshi
authors.initials: T
authors.lastname: Tsubata
authors.forename: Hideharu
authors.initials: H
authors.lastname: Ishida
authors.forename: Makoto
authors.initials: M
authors.lastname: Kiso
mesh_terms: D000818:Animals; D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D004187:Disaccharides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D019158:N-Acetylneuraminic Acid / Q000737:chemistry*; D051918:Sialic Acid Binding Ig-like Lectin 2 / Q000737:chemistry* / Q000378:metabolism
chemical_list: D001713:Biphenyl Compounds; D004187:Disaccharides; D051918:Sialic Acid Binding Ig-like Lectin 2; D019158:N-Acetylneuraminic Acid