Medium-firm drug-candidate library of cryptand-like structures on T7: Design and selection of strong binder for Hsp90

Le résumé fourni par la source

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 10^9 diversity, we obtained a binder toward a cancer-related protein (Hsp90) with an antibody-like strong affinity (K_D = 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).

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