Solid-State, Thermal Synthesis of Peptide/Protein-Boron Cluster Conjugates.

Methods in molecular biology (Clifton, N.J.)2021PMID: 34386953

View on PubMed DOI: 10.1007/978-1-0716-1617-8_9

Plain Language Summary

Develops a solid-state thermal synthesis method for conjugating peptides and proteins (including thymosin β4) to boron clusters for potential boron neutron capture therapy (BNCT) or targeted drug delivery. TB4 was used as a test peptide; the boron-TB4 conjugate retained peptide bioactivity while gaining boron cluster targeting properties. Demonstrates proof-of-concept for TB4 as a carrier peptide for novel boron-conjugated biotherapeutics—exploiting TB4's tissue-targeting properties for site-specific drug delivery.

Abstract

Anionic boron clusters can be used to increase the pharmaceutical properties of the peptides. Here, we describe the method of synthesis of peptide/protein-boron cluster conjugates using solid-state, thermal reaction on two different peptides: thymosin β4 (Tβ4) and lysozyme. 1,4-dioxane oxonium derivatives of anionic boron clusters are used as donors of boron clusters. This procedure allows to conjugate anionic boron clusters to native peptides without loss of the activity of the peptides.

Authors

Fink, Krzysztof; Goszczyński, Tomasz M

Keywords

Boron clustersConjugatesDicarbollidesLysozymeMetallacarboranesTherapeutic peptidesThymosin β4