title: "Click" saccharide/beta-lactam hybrids for lectin inhibition.
abstract: Hybrid glycopeptide beta-lactam mimetics designed to bind lectins or carbohydrate recognition domains in selectins have been prepared according to a "shape-modulating linker" design. This approach was implemented using the azide-alkyne "click" cycloaddition reaction, and as shown by NMR/MD experiments, binding of the resulting mimetics to Ulex Europaeus Lectin-1 (UEL-1) occurred after a "bent-to-extended" conformational change around a partially rotatable triazolylmethylene moiety.
authors.affiliation: Departamento de Química Orgánica-I, Universidad del País Vasco, Joxe Mari Korta R& D Center, San Sebastián, Spain.
authors.forename: Claudio
authors.initials: C
authors.lastname: Palomo
authors.forename: Jesus M
authors.initials: JM
authors.lastname: Aizpurua
authors.forename: Eva
authors.initials: E
authors.lastname: Balentová
authors.forename: Itxaso
authors.initials: I
authors.lastname: Azcune
authors.forename: J Ignacio
authors.initials: JI
authors.lastname: Santos
authors.forename: Jesús
authors.initials: J
authors.lastname: Jiménez-Barbero
authors.forename: Javier
authors.initials: J
authors.lastname: Cañada
authors.forename: José Ignacio
authors.initials: JI
authors.lastname: Miranda
mesh_terms: D040761:Biomimetic Materials / Q000737:chemistry / Q000494:pharmacology; D006020:Glycopeptides / Q000737:chemistry* / Q000494:pharmacology*; D037102:Lectins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D010940:Plant Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry; D011487:Protein Conformation; D039762:Ulex / Q000737:chemistry; D047090:beta-Lactams / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D006020:Glycopeptides; D037102:Lectins; D010940:Plant Proteins; D047090:beta-Lactams