Hitting the Target: Novel Reagents for the Chemical-Proteomics Based Identification of Vascular Accessible Biomarkers

摘要

A promising approach for the development of novel cancer therapeutics with fewer side effects in healthy tissues is the targeted delivery of bioactive molecules directly to the site of disease. The identification of vascular accessible, tumor specific target proteins is a prerequisite for therapeutic or diagnostic purposes. To analyze the vascular accessible proteome via mass spectrometry, the respective proteins have to be specifically enriched. One avenue towards the enrichment of vascular accessible proteins is their modification with membrane-impermeable ester-derivatives of biotin, which can be used for streptavidin-based enrichment. This project focuses on the development of two novel peptide-based biotinylation reagents with high reactivity and selectivity for vascular accessible proteins. Their reactivity is tested on single proteins, followed by in vitro and in vivo validation performed in comparison to commercially available biotinylation reagents.