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Updated: Jun 7, 2025

Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay
Published on: February 28, 2025
ARCaDia: single-round screening of a DNA-type targeted covalent binder possessing a latent warhead
Masumi Taki1,2, Masayasu Kuwahara3, Chaohui Li1
1Department of Engineering Science, The Graduate School of Informatics and Engineering, The University of Electro-Communications (UEC), 1-5-1 Chofugaoka, Chofu, Tokyo 182-8585, Japan. taki@pc.uec.ac.jp.
Abstract:
A covalent binder for a target protein was obtained by a direct single-round screening of a latent-warhead-modified DNA library via affinity/reactivity-based co-selection of aptameric deoxyribonucleic acid (ARCaDia), followed by a top k-mer analysis. The optimal position of the conjugated warhead on the selected aptamer was simultaneously identified.
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