Publications by authors named "Jacopo Gomena"
Targeted tumour therapy has proved to be an efficient alternative to overcome the limitations of conventional chemotherapy. The upregulation of the bombesin receptor 2 (BB2) in several malignancies and the advantages offered by peptide drug conjugates over antibody drug conjugates in terms of production and tumour targeting motivated us to synthesise and test bombesin conjugates armed with the tubulin binder monomethyl auristatin E. The widely used Val-Cit-PABC was initially included as cathepsin cleavable self-immolative linker for the release of the free drug.
View Article and Find Full Text PDFChemotherapy is still one of the main therapeutic approaches in cancer therapy. Nevertheless, its poor selectivity causes severe toxic side effects that, together with the development of drug resistance in tumor cells, results in a limitation for its application. Tumor-targeted drug delivery is a possible choice to overcome these drawbacks.
View Article and Find Full Text PDFArticle Synopsis
- Targeted tumor therapy shows promise as a better alternative to traditional chemotherapy, especially by focusing on receptors like gastrin-releasing peptide receptor (GRP-R) which are overexpressed in various cancers.
- Researchers developed eleven daunorubicin-containing peptide-drug conjugates that effectively deliver the drug to prostate and breast cancer cells using bombesin analogues as targeting agents.
- Two of these conjugates demonstrated strong anti-cancer effects, successfully reducing tumor volume in live subjects while maintaining a safe profile and high stability in the bloodstream.