TRPV1-targeted ligand-drug conjugates to treat prostate cancer

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Cancer remains a leading cause of death and morbidity worldwide. Prostate cancer (PC) is among the most frequently diagnosed non-skin cancers. Despite major advances in the understanding of cancer biology and development of candidate therapeutic agents, there is still an urgent need of exploiting innovative chemotypes and disrupting novel signalling pathways. Evidence suggests that targeted therapies may provide an original means of selectively modulating diseased prostate cells. Herein we propose the validation and devlopment of an unprecedented approach to tackle PC, addressing the overexpressed transient receptor potential vanilloid channel V1 (TRPV1) with ligand-drug conjugates. This strategy provides a pioneering technological advance by aiming at the disruption of calcium signalling, while selectively targeting cancer cells for the delivery of cytotoxic payloads. The approach will additionally yield chemical probes for studying TRPV1 biology and for whole-animal optical imaging of TRPV1-overexpressed cancer cells.