Activatable molecular agents for cancer theranostics

Abstract

Theranostics that integrates diagnosis and treatment modalities has attracted great attention due to its abilities of personalized therapy and real-time monitoring of therapeutic outcome. Such a theranostic paradigm requires agents to simultaneously possess the capabilities of targeting, imaging, and treatment. Activatable molecular agents (AMAs) are promising for cancer theranostics, as they show a higher signal-to-noise ratio (SNR), real-time detection of cancer-associated biomarkers, lower normal tissue toxicity, and a higher therapeutic effect. This perspective summarizes the recent advancements of AMAs, which include imagingguided chemotherapy, imaging-guided photodynamic therapy, and imaging-guided photothermal therapy.The molecular design principles, theranostic mechanisms, and biomedical applications of AMAs are described, followed by a discussion of potential challenges of AMAs in cancer theranostics.

Fine-tuning the electronic structure of heavy-atom-free BODIPY photosensitizers for fluorescence imaging and mitochondria-targeted photodynamic therapy

“…2,3 In particular, theranostics has recently been recognized as a promising medical technology that combines diagnostic and therapeutic capabilities in one dose to achieve the real-time and precise monitoring of the therapeutic effect of the drug. 4 Moreover, PDT combined with image-guided diagnosis has attracted considerable attention owing to its prominent advantages such as high spatiotemporal selectivity, noninvasiveness, and fewer side effects. [5][6][7] Therefore, the design of novel PSs that can effectively produce both uorescence and ROS is in high demand.…”

Recent advances in construction of small molecule-based fluorophore-drug conjugates

“…As shown in Fig. 4 , in most designs, upon successful cellular delivery of the cleavable conjugate, due to specific microenvironment in tumor or target cells, the conjugate could be designed to undergo controlled degradation in order to release free drug molecules (traceless release) and simultaneously generate an easy-to-monitor fluorescent signal [ 42 , 43 ], thus achieving “on-demand” therapy. The choice of cleavable linkers should be chosen so that they are stable during organic synthesis but highly labile (and specific) toward the expected cleavage conditions.…”

Recent Advances in Crosslinked Nanogel for Multimodal Imaging and Cancer Therapy

“…Compared with conventional nanogels-based drug-delivery systems (DDS), nanogels with environmental responsiveness may be a better choice for DDS development. The tumor microenvironment has features such as acidic pH, reactive oxygen species (ROS) and GSH overexpression [ 12 ]. Thus, development of nanogels which can response to these features is feasible method in DDS design.…”

“…Recently, phototheranostics, which based on optical imaging, have been widely studied because of their unique advantages such as high safety and sensitivity, low cost and capability of multi-channel imaging [ 7 , 8 , 9 , 10 , 11 ]. Numerous phototheranostic systems based on variety of materials such as small molecular dyes [ 12 , 13 ], anti-cancer drugs [ 14 , 15 ] and biomacromolecules [ 16 ] have been developed. However, as theranostics require the combination of multiple functionalities including imaging and therapy, complicated synthetic procedures are usually inevitable [ 17 , 18 ].…”