1. Characterization of DNA-conjugated compounds using a regenerable chip.
- Author
-
Lin W, Reddavide FV, Uzunova V, Gür FN, and Zhang Y
- Subjects
- Biosensing Techniques, Combinatorial Chemistry Techniques, Cyclophilins metabolism, Cyclosporine metabolism, DNA metabolism, Drug Design, Drug Discovery, Gene Library, Humans, Immunosuppressive Agents metabolism, Kinetics, Oligonucleotide Array Sequence Analysis, Small Molecule Libraries metabolism, Structure-Activity Relationship, Cyclophilins chemistry, Cyclosporine chemistry, DNA chemistry, Immunosuppressive Agents chemistry, Small Molecule Libraries chemistry
- 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.
- Published
- 2015
- Full Text
- View/download PDF