Bioconjugates to specifically render inhibitorswater-soluble

Abstract

Polymer–peptide conjugates are utilised to render small-molecule inhibitors of the kinase IspE, a promising new antimalarial target, water-soluble. It is shown that the peptide sequence of poly(ethylene oxide)–peptide conjugates can be tailored to mediate specific interactions with the ligands, allowing the solubilisation of even highly challenging inhibitors. This strategy avoids compromising the inhibitor structure to afford water solubility and potentially enables the exploration of a greater structural space of both inhibitors and drugs.