title: Click-enabled heterotrifunctional template for sequential bioconjugations.
abstract: A heterotrifunctional template was developed that utilizes thiol-maleimide and click chemistries (both copper-free and copper-mediated) to effect sequential biomolecule conjugations in a one-pot process. The breadth of compatible substrates was illustrated through highly efficient conjugations of protein, peptide, sugar, lipid, fluoroalkane, biotin and fluorophore molecules. This template should be useful for the creation of chemically-enhanced/enabled biotherapeutics, especially through the expression of discontinuous (and heterogeneous) epitopes.
authors.affiliation: Chemical Biology Group, Worldwide Medicinal Chemistry, Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. dmb38@kent.ac.uk
authors.forename: David M
authors.initials: DM
authors.lastname: Beal
authors.forename: Victoria E
authors.initials: VE
authors.lastname: Albrow
authors.forename: George
authors.initials: G
authors.lastname: Burslem
authors.forename: Louisa
authors.initials: L
authors.lastname: Hitchen
authors.forename: Carla
authors.initials: C
authors.lastname: Fernandes
authors.forename: Cris
authors.initials: C
authors.lastname: Lapthorn
authors.forename: Lee R
authors.initials: LR
authors.lastname: Roberts
authors.forename: Matthew D
authors.initials: MD
authors.lastname: Selby
authors.forename: Lyn H
authors.initials: LH
authors.lastname: Jones
mesh_terms: D000818:Animals; D002417:Cattle; D057930:Click Chemistry; D008958:Models, Molecular; D011487:Protein Conformation; D011506:Proteins / Q000737:chemistry*; D012710:Serum Albumin, Bovine / Q000737:chemistry; D013237:Stereoisomerism
chemical_list: D011506:Proteins; D012710:Serum Albumin, Bovine