title: Topological templates as tool in molecular recognition and peptide mimicry: synthesis of a TASK library.
abstract: Topological templates disposing orthogonally protected reactive sites in defined spatial positions of a variable degree of flexibility can serve as a pool for the selective functionalization by groups thought to interact with an acceptor molecule. This strategy is exemplified by the chemo-selective ligation of amino-acid residues to a cyclic peptide as a structural motif (template-assembled side chains; TASK) applying the concept of combinatorial libraries. Binding assays to a monoclonal antibody allow for the delineation of a lead compound mimicking the structural features of a discontinuous epitope. The conceptually novel approach may serve as a tool in molecular recognition studies and in drug development.
authors.affiliation: Section de Chimie, Université de Lausanne, Switzerland.
authors.forename: U
authors.initials: U
authors.lastname: Sila
authors.forename: M
authors.initials: M
authors.lastname: Mutter
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D000911:Antibodies, Monoclonal; D002846:Chromatography, Affinity; D002851:Chromatography, High Pressure Liquid; D016208:Databases, Factual; D051379:Mice; D008807:Mice, Inbred BALB C / Q000276:immunology; D008958:Models, Molecular; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000302:isolation & purification; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000302:isolation & purification; D011487:Protein Conformation; D013329:Structure-Activity Relationship
chemical_list: D000911:Antibodies, Monoclonal; D009842:Oligopeptides; D010455:Peptides