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Issue 1, 2021
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A medium-firm drug-candidate library of cryptand-like structures on T7 phage: design and selection of a strong binder for Hsp90

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Abstract

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).

Graphical abstract: A medium-firm drug-candidate library of cryptand-like structures on T7 phage: design and selection of a strong binder for Hsp90

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Article information


Submitted
08 Sep 2020
Accepted
12 Oct 2020
First published
14 Oct 2020

Org. Biomol. Chem., 2021,19, 146-150
Article type
Communication

A medium-firm drug-candidate library of cryptand-like structures on T7 phage: design and selection of a strong binder for Hsp90

K. Mochizuki, L. Matsukura, Y. Ito, N. Miyashita and M. Taki, Org. Biomol. Chem., 2021, 19, 146
DOI: 10.1039/D0OB01855D

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