Bladder Cancer Photodynamic Therapeutic Agent with Off‐On Magnetic Resonance Imaging Enhancement. Issue 11 (16th August 2019) - Xie, Chen
Abstract: Acting as an extracellular matrix protein receptor, αV β3 integrin becomes an appealing target for photodynamic therapy of bladder cancer. Here, specific αV β3 ‐integrin‐targeting porphyrinato‐gadolinium complexes (Gd‐PEG‐R n ) are demonstrated as off‐on theranostic agents, where R n are specific peptides. Among them, Gd‐PEG‐R 3 shows both impressive phototherapeutic index and robust in vivo magnetic resonance imaging (MRI) signal enhancement. Significant selectivity of Gd‐PEG‐R 3 is proven by its high αV β3 integrin binding affinity in positive bladder cancer cells. All these findings support Gd‐PEG‐R 3 as a promising bi‐functional medical agent with both MRI contrasting ability and photodynamic therapeutic potential for curing bladder cancer. Abstract : Gadolinium‐based porphyrin complexes, after conjugating with bladder‐cancer‐specific peptides, show both diagnostic and therapeutic effects simultaneously: the complexes have increasing relaxivity after binding with targets and help improve magnetic resonance imaging quality; photodynamic therapy can also be achieved by light trigger and singlet oxygen generation afterward with high selectivity to bladder cancers.