| Report number | MED-033 |
| Title | Dual Tumor Targeting Based on a pH Sensitive Peptide Platform |
| Author(s) | Campello, Maria Paula Cabral (C2TN) ; Paulo, Antonio (C2TN) ; Gano, Lurdes (C2TN) ; Fernandes, Celia (C2TN) |
| Publication | 2023 |
| Imprint | 2023-03-09 |
| Number of pages | 4 |
| Keywords | radiopharmaceutical; targeted radiopeptide therapy; theranostics; MEDICIS; 155Tb; |
| Abstract | Nowadays it is well established that the microenvironment of solid tumors is associated with increased metabolic activity and hypoxia resulting in an elevated extracellular acidity. Acidosis is associated with tumor development both at very early and at advanced stages, being a tumor property that may serve as a general biomarker. Due to overexpression of many peptide receptors in several tumors, radiolabeled receptor-specific peptides have become of utmost importance as targeting vectors for the design and development of new diagnostic and therapeutic radiopharmaceuticals. We propose to evaluate the ability of a multifunctional pHLIP-based platform for selective delivery and release of imaging or therapeutic radioactive units to tumor cells. This multifunctional construct contains two targeting tumor vectors: a pHLIP peptide for introducing and releasing the radioactive unit into the acidic tumor cell, and an antagonist somatostatin derivative to give specificity to the construct towards receptors tumor cells, without triggering internalization. The main goal of the project is to synthesize, characterize and biologically evaluate these novel constructs that comprises a chelator, for stabilization of trivalent radiometals (radioactive unit), a peptide for introducing and releasing the radioactive unit into the tumour cell, and a somatostatin peptide antagonist to provide cell membrane specificity towards somatostatin receptors, which are overexpressed in many neuroendocrine tumours. |
| Submitted by | thierry.stora@cern.ch |
Record created 2023-03-17, last modified 2023-03-17
