Targeting the transporters of cationic amino acids for cancer radiotheranostics: experimental and computational chemistry approach

Overview

Project Summary

Radiolabeled amino acid derivatives for assessment of increased rates of amino acid transport in cancer cells continue to gain importance in cancer imaging. Radiotracers targeting transporters of cationic amino acids hold great potential as imaging biomarkers for predicting and monitoring response to arginine deprivation therapy or imaging brain tumors, among others. No metal-based radiotracers are known, especially those based on radiometals obtained from widespread commercially available generators. Aimed at addressing unmet needs in the clinical setting, we will explore a new family of radiometallated cationic amino acid derivatives for cancer theranostics combining an experimental approach with computational chemistry tools. We expect that this integrated method will shade light on the structural factors that influence the transporter-recognizing properties of the radiotracers and help in the design of new compounds with improved imaging and therapeutic properties (Theranostics).

Main Goals

The outcome of the combined experimental and in silico approaches will enable the rationalization of the overall results and to identify the structural features that influence the affinity of the (radio)metal complexes for the transporters binding sites. In this way, alterations to the lead compounds can be proposed, which will ultimately result in the design of metal complexes with improved cationic amino acids transporter-recognizing properties and higher potential for cancer theranostics.

Project Details