title: Characterization of DNA-conjugated compounds using a regenerable chip.
abstract: DNA-encoded chemical library (DECL) technology has emerged as a new avenue in the field of drug discovery. Combined with high-throughput sequencing, DECL selection experiments can provide not only many lead compounds but also insights into the structure-affinity relationship. However, the counts of individual DNA codes reflect, but cannot be used to precisely rank, the binding affinities of the corresponding compounds to protein targets. Herein, we describe a chip-based approach to realize an automated high-throughput assay for the kinetic characterization of the interaction between DNA-conjugated small organic compounds and protein targets. Importantly, this method can be applied to both single-pharmacophore DECLs and self-assembled dual-pharmacophore DECLs.
authors.affiliation: B CUBE Center for Molecular Bioengineering, Technische Universität Dresden , 01307 Dresden, Germany.
authors.forename: Weilin
authors.initials: W
authors.lastname: Lin
authors.forename: Francesco V
authors.initials: FV
authors.lastname: Reddavide
authors.forename: Veselina
authors.initials: V
authors.lastname: Uzunova
authors.forename: Fatih Nadi
authors.initials: FN
authors.lastname: Gür
authors.forename: Yixin
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D015374:Biosensing Techniques; D020650:Combinatorial Chemistry Techniques; D021983:Cyclophilins / Q000737:chemistry* / Q000378:metabolism; D016572:Cyclosporine / Q000737:chemistry* / Q000378:metabolism; D004247:DNA / Q000737:chemistry* / Q000378:metabolism; D015195:Drug Design; D055808:Drug Discovery; D015723:Gene Library; D006801:Humans; D007166:Immunosuppressive Agents / Q000737:chemistry* / Q000378:metabolism; D007700:Kinetics; D020411:Oligonucleotide Array Sequence Analysis; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D007166:Immunosuppressive Agents; D054852:Small Molecule Libraries; D016572:Cyclosporine; D004247:DNA; D021983:Cyclophilins