Every year, over 8 million people die worldwide due to cancer. Proteasome inhibitors have promising anticancer activity and are being explored for their therapeutic potential. Peptide-boronic acids (PBA) such as Bortezomib, an FDA approved therapy for multiple myeloma, show potent proteasome inhibition but synthesis can be costly, inefficient, and not conducive to developing large libraries of derivatives. To improve synthetic access to derivatives of Bortezomib and other PBAs, a method for recyclable solid-phase peptide synthesis was investigated, examining the use of different polystyrene resins as solid-support. Ability of the resins to withstand peptide synthesis conditions and to be effectively recycled for use in further syntheses was probed. Upon optimization of the resin, a synthetic method for Bortezomib on solid-support was developed and optimized. This synthetic method will be applied to developing large libraries of derivatives of Bortezomib and other PBAs.

Recyclable solid-support for the synthesis of boronic acid-modified peptides

2019 Spring National Meeting

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