Photochemical reactions have been the subject of renewed interest over the last two decades, leading to the development of many new,d iversea nd powerful chemical transformations. More recently,t hese developments have been expanded to enable the photochemical macrocyclisation of peptidesa nd small proteins. These constructs benefit from increased stability, structuralr igidity and biological potency over their linear counterparts, providing opportunities for improved therapeutica gents. In this review,a no verview of both the established and emerging methods for photochemicalp eptide macrocyclisation is presented, highlighting both the limitations and opportunities for further innovation in the field.
Ortho-boronoaldehydes react with amine-based nucleophiles with dramatically increased rates and product stabilities, relative to unfunctionalised benzaldehydes, leading to exciting applications across biological and material chemistry. We have developed a novel...
Ortho-boronoaldehydes react with amine-based nucleophiles with dramatically increased rates and product stabilities, relative to unfunctionalised benzaldehydes, leading to exciting applications across biological and material chemistry. We have developed a novel Förster resonance energy transfer (FRET)-based assay to provide key new insights into the reactivity of these boronoaldehydes, allowing us to track conjugation with unprecedented sensitivity and accuracy under standardised conditions. Our results highlight the key role played by reaction pH, buffer additives, and boronoaldehyde structure in controlling conjugation speed and stability, providing design criteria for further innovations and applications in the field.
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