Targeted 1,3-dipolar cycloaddition with acrolein for cancer prodrug activation

Abstract

Prodrug activation strategy by utilizing the reaction between aryl azide and endogenous acrolein that is generally overproduced by cancer cells.

Mutual leveraging of proximity effects and click chemistry in chemical biology

“…To the best of our knowledge, the first example of a bioorthogonal prodrug appeared in 2008 127 . A decade later, a handful of bioorthogonal prodrugs using new chemistry have been reported based on a limited pool of click reactions with bond cleavage characteristics 10,128–131 . In 2019, we devised a new “click, cyc lize and release” system for building bioorthogonal prodrugs.…”

“…127 A decade later, a handful of bioorthogonal prodrugs using new chemistry have been reported based on a limited pool of click reactions with bond cleavage characteristics. 10,[128][129][130][131] In 2019, we devised a new "click, cyc lize and release" system for building bioorthogonal prodrugs. In contrast to using the bond cleavage nature of some click reactions for prodrug design, we leveraged the bond formation nature of a DA reaction, which recruits a nucleophile to the close proximity of an existing electrophile to enable cyclization-based release of the drug payload.…”

A supramolecular nanoplatform for imaging-guided phototherapies via hypoxia tumour microenvironment remodeling

“…[1][2][3] To reduce the pain caused by cancer both physically and psychologically, a series of therapeutic methods have been developed, such as surgical treatment, chemotherapy, and radiotherapy. [4][5][6][7] Among them, phototherapy, which leads to almost no drug-resistance and no signicant side effects to surrounding tissues, has received increasing attention. [8][9][10] Photodynamic therapy (PDT) relies on that upon light irradiation, photosensitizers transfer the energy or electrons to oxygen molecules to produce singlet oxygen ( 1 O 2 ), and it emerged as a promising and invasive potential alternative therapy.…”

Flucytosine‐based prodrug activation by cold physical plasma

“…[24][25][26] To date, numerous prodrug types and their activation mechanisms have been investigated. [27][28][29][30][31] These strategies were founded based on exploiting the cancer characteristic environment (internal stimuli): for example, acidic extracellular pH level, high redox homeostasis due to high levels of reactive species such as H 2 O 2 and peroxynitrite, and overexpressed enzymes. External stimuli such as light, ultrasound, and heat could also be applied to trigger a controlled prodrug activation and liberation of the active drug.…”