Proteolysis-targeting chimera (PROTAC) nanomedicines toward cancer treatment: From synthesis to therapeutic delivery [PDF]
BiomaterialsProteolysis-targeting chimera (PROTAC) has emerged as a groundbreaking therapeutic strategy by hijacking the endogenous ubiquitin proteasome system (UPS) for targeted protein degradation. These heterobifunctional molecules recruit E3 ligases to recognize
Fuwu Zhang, Xiaoyuan Chen, Xiao Zhang
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Promising Proteolysis-Targeting Chimera for Mutant p53-R175H [PDF]
ACS OmegaThe tumor suppressor protein p53 is among the most commonly mutated proteins across a variety of cancer types. Notably, the p53 R175H mutation ranks as one of the most prevalent hotspot mutations. Proteolysis-targeting chimeras (PROTACs) represent a class of bifunctional molecules capable of harnessing the cellular ubiquitin-proteasome pathway to ...
Xinzhe Zhuang +6 more
doaj +4 more sources
The clinical advances of proteolysis targeting chimeras in oncology [PDF]
Exploration of Targeted Anti-tumor Therapy, 2021 Proteolysis targeting chimeras (PROTACs) are a class of small molecules designed to target proteins for degradation. Their novel and unique modes of action provide PROTACs with the potential for their application in the management of both solid and ...
Hao Xie +3 more
doaj +3 more sources
Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy [PDF]
Journal of Hematology & Oncology, 2020 Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently ...
Xin Li, Yongcheng Song
doaj +2 more sources
Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity [PDF]
Nature Communications, 2020 Senolytics have the potential to extend healthspan by selectively killing senescent cells (SCs), but senolytics that target Bcl-xl may cause platelet toxicity.
Yonghan He +21 more
doaj +2 more sources
Natural product-based PROteolysis TArgeting Chimeras (PROTACs)
Natural Product Reports, 2022 Natural products exert their action by direct interaction with specific protein targets. Thus, they provide valuable starting points for the design of novel PROTAC molecules, as they present biologically pre-validated protein–ligand pairs.
Miaomiao Liu +2 more
openaire +6 more sources
Current Status of Oligonucleotide-Based Protein Degraders
Pharmaceutics, 2023 Transcription factors (TFs) and RNA-binding proteins (RBPs) have long been considered undruggable, mainly because they lack ligand-binding sites and are equipped with flat and narrow protein surfaces. Protein-specific oligonucleotides have been harnessed
Po-Chang Shih +3 more
doaj +2 more sources
Proceedings, 2019 Proteolysis targeting chimera molecules (PROTACS) are heterobifunctional small moleculesdesigned to induce intracellular protein degradation [...]
Carles Galdeano
doaj +2 more sources
Design and Synthesis of Polyamine‐Proteolysis Targeting Chimera Conjugates for Histone Deacetylase (HDAC) Degradation with Enhanced Cellular Uptake [PDF]
ChemistryOpenAlthough histone deacetylase (HDAC) inhibitors have demonstrated significant advantages in the field of targeted cancer therapy, numerous adverse events have been observed due to the high doses required to achieve therapeutic effects.
Yanran Liu +6 more
doaj +2 more sources
Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells
Nature Communications, 2021 Targeting regulatory T cells (Treg) represents a therapeutic option to abrogate tumor-associated immune suppression. Here the authors show that pharmacological degradation of BCL-XL preferentially induces apoptosis of tumor-infiltrating Treg, promoting ...
Ryan Kolb +18 more
doaj +2 more sources