Successful manual synthesis of TD2.2 peptide acting as a blood-brain barrier shuttle has been achieved. TD2.2 was successfully synthesised by sequential condensation of four protected peptide fragments on solid-phase settings after several unsuccessful attempts using the stepwise approach. These fragments were chosen to minimize the number of demanding amino acids (in terms of coupling, Fmoc-removal) in each fragment that are expected to hamper the overall synthetic process. Thus, the hydrophobic amino acids as well as Arg(Pbf) were strategically spread over multiple fragments rather than having them congested in one fragment.<br/>This study demonstrates how a peptide that shows big challenges in the synthesis using the common stepwise elongation methodology, can be synthesised with an acceptable purity. It also emphasizes that choosing the right fragment with certain amino acid constituents is key for a successful synthesis. It is worth highlighting that lower amount of reagents was required to synthesise the final peptide with an identical purity to that obtained by the automatic synthesiser.

Successful synthesis of glial-specific blood-brain barrier shuttle peptide following fragment condensation approach on solid-phase resin

Where thousands of chemistry professionals meet to share ideas and advance scientific and technical knowledge. Spring 2023 abstracts, posters, and presentations will launch at the end of March.

ACS Spring 2023

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.