Tailoring albumin-based theranostic PROTACs nanoparticles for enhanced NIR-II bioimaging and synergistic cancer chemo-phototherapy

Nano-PROTACs: state of the art and perspectives

“…7A). [78][79][80][81] Considering this, Chen et al 78 conjugated oleic acid to the ligand of E3 ligase through different alkyl linkers to screen the most effective chimera (Fig. 7B).…”

New-generation advanced PROTACs as potential therapeutic agents in cancer therapy

“…J Chemical structures of the structure of the nano-PROTACs (adapted from [ 144 ]). K Chemical structures of the structure of the nano-PROTACs (adapted from [ 145 ]). L Chemical structures of the structure of the nano-PROTACs (adapted from [ 146 ]).…”

“…Hu et al . reported a PROTAC-Cy7, tridentate molecular probe, using a three-in-one molecular design strategy, which incorporated the E3 ligase ligand pomalidomide, a warhead targeting MCL-1, and a heptamethine cyanine linkage connecting the warhead and the ligand within the same scaffold [ 145 ]. To overcome water insolubility, bovine serum albumin (BSA) nanoparticles with exceptional biocompatibility, nonantigenicity, and biosafety were employed to encapsulate PROTAC-Cy7.…”

Enhanced Tumor Targeting and Penetration of Proteolysis-Targeting Chimeras through iRGD Peptide Conjugation: A Strategy for Precise Protein Degradation in Breast Cancer

“…Compared to conventional small molecule inhibitors, PROTACs demonstrate significant advantages in targeting undruggable proteins, enhancing selectivity, and overcoming resistance. − However, PROTACs also possess inherent limitations . The relatively large size of PROTAC molecules often results in poor water solubility and cell membrane permeability. , Additionally, the inability to achieve the tissue-selective degradation of PROTACs may pose a potential challenge for further clinical applications. Extensive research has been devoted to addressing the issues of targeted delivery associated with PROTACs, such as antibody-conjugated PROTACs and folate-conjugated PROTACs, resulting in improved tumor tissue selectivity. − Nevertheless, the development of targeted PROTACs still faces significant challenges such as potential immunogenicity, inconvenient synthesis, and limited aqueous solubility. ,, More importantly, overcoming increased interstitial pressure in tumor tissues and penetrating the vascular barrier to access the tumor parenchyma remain major challenges in PROTAC-based drug research.…”

“…6 The relatively large size of PROTAC molecules often results in poor water solubility and cell membrane permeability. 7,8 Additionally, the inability to achieve the tissue-selective degradation of PROTACs may pose a potential challenge for further clinical applications. Extensive research has been devoted to addressing the issues of targeted delivery associated with PROTACs, such as antibody-conjugated PROTACs and folate-conjugated PROTACs, resulting in improved tumor tissue selectivity.…”