title: Multifunctional multivalency: a focused library of polymeric cholera toxin antagonists.
abstract: Structural pre-organization of the multivalent ligands is important for successful interaction with multimeric proteins. Polymer-based heterobifunctional ligands that contain pendant groups prearranged into heterodimers can be used to probe the active site and surrounding area of the receptor. Here we describe the synthesis and activities of a series of galactose conjugates on polyacrylamide and dextran. Conjugation of a second fragment resulted in nanomolar inhibitors of cholera toxin, while the galactose-only progenitors showed no detectable activity.
authors: Alberta Ingenuity Centre for Carbohydrate Science, Department of Chemistry, University of Alberta, Edmonton, Alberta, Canada.
authors: Huu-Anh
authors: HA
authors: Tran
authors: Pavel I
authors: PI
authors: Kitov
authors: Eugenia
authors: E
authors: Paszkiewicz
authors: Joanna M
authors: JM
authors: Sadowska
authors: David R
authors: DR
authors: Bundle
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000586:Amination; D001665:Binding Sites; D002772:Cholera Toxin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D003911:Dextrans / Q000737:chemistry; D055808:Drug Discovery; D004797:Enzyme-Linked Immunosorbent Assay; D005677:G(M1) Ganglioside / Q000378:metabolism; D005690:Galactose / Q000737:chemistry; D008024:Ligands; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D000099166:Polyacrylamides
chemical_list: D000180:Acrylic Resins; D002772:Cholera Toxin; D003911:Dextrans; D005677:G(M1) Ganglioside; D005690:Galactose; D008024:Ligands; D011108:Polymers; D000099166:Polyacrylamides