研究業績リスト
ジャーナル論文 - rm_published_papers: Scientific Journal
ARCaDia: single-round screening of a DNA-type targeted covalent binder possessing a latent warhead
公開済 12/2024
Chemical Communications, 60, 100, 14964 - 14967
A covalent binder was identified using a single-round screening from a latent-warhead-modified DNA library, coupled with top k-mer analysis to pinpoint the optimal warhead position on the aptamer.
ジャーナル論文 - rm_misc: Introduction Scientific Journal
Peptidic Targeted Covalent Inhibitors (TCIs) possessing Stability in Serum
公開済 04/2024
PEPTIDE NEWSLETTER JAPAN, 132, 4 - 6
ジャーナル論文 - rm_published_papers: Scientific Journal
公開済 02/2023
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 24, 4
ジャーナル論文 - rm_published_papers: Scientific Journal
Relative Nuclease Resistance of a DNA Aptamer Covalently Conjugated to a Target Protein
公開済 14/07/2022
International Journal of Molecular Sciences, 23, 7778
ジャーナル論文 - rm_published_papers: Scientific Journal
公開済 04/06/2022
Anal. Bioanal. Chem, 414, 4803 - 4807
ジャーナル論文 - rm_published_papers: Scientific Journal
Covalent Biologics：中・高分子型共有結合性薬剤
公開済 11/2021
ファルマシア, 57, 11, 1019 - 1024
ジャーナル論文 - rm_published_papers: Scientific Journal
公開済 22/04/2021
生物工学会誌, 99, 4, 172 - 175
ジャーナル論文 - rm_published_papers: Scientific Journal
公開済 11/03/2021
Chem. Commun, 57, 20, 2483 - 2486
Alleviating the potential risk of irreversible adverse drug effects has been an important and challenging issue for the development of covalent drugs. Here we created a DNA-aptamer-type covalent drug by introducing a sulfonyl fluoride warhead at appropriate positions of the thrombin binding aptamer to create weaponized covalent drugs. We showed the de-activation of thrombin by the novel modality, followed by its re-activation by the complementary strand antidote at an arbitrary time. We envision that such on-demand reversal of covalent drugs will alleviate the major concern of potentially irreversible ADEs and accelerate the translational application of covalent aptamer drugs.
ジャーナル論文 - rm_published_papers: Scientific Journal
公開済 07/01/2021
Org. Biomol. Chem, 19, 1, 146 - 150
We designed and synthesized a medium-firm drug-candidate library of cryptand-like structures possessing a randomized peptide linker on the bacteriophage T7. From the macrocyclic library with a 109 diversity, we obtained a binder toward a cancer-related protein (Hsp90) with an antibody-like strong affinity (KD = 62 nM) and the binding was driven by the enthalpy. The selected supramolecular ligand inhibited Hsp90 activity by site-specific binding outside of the well-known ATP-binding pocket on the N-terminal domain (NTD).
ジャーナル論文 - rm_published_papers: Scientific Journal
公開済 2021
Chemical Communications, 57, 44, 5378 - 5381
To find targeted covalent biologics, we demonstrated a direct screening method of a peptidic covalent binder via reactivity/affinity-based co-selection using T7 phage display.