Peptides and other bRO5 compounds have become thoroughly entrenched within the medicinal chemist’s modality toolbox given their potential for antibody-like target affinity and specificity coupled with cell permeability.  With the advent of unbiased screening technologies, incorporating both natural and non-natural amino acids, the propensity for pursing a discovery project with these compounds has also increased.  Once hits are selected from the primary screen, the chemist’s job truly begins.  Herein, we will present highly parallel synthesis strategies enabling reliable synthesis on minimal scale and discuss methods which enable peptide cleanup in parallel, further streamlining delivery for evaluation.

Streamlining hit-to-lead optimization: Automating highly parallel peptide synthesis and cleanup

ACS Fall 2021

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