ac503960z_si_001.pdf (1.69 MB)
Characterization of DNA-Conjugated Compounds Using a Regenerable Chip
journal contribution
posted on 2015-01-20, 00:00 authored by Weilin Lin, Francesco
V. Reddavide, Veselina Uzunova, Fatih Nadi Gür, Yixin ZhangDNA-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.