Specific proteolysis mediated by a p97-directed proteolysis-targeting chimera (p97-PROTAC) [PDF]
eLifeThe p97 protein is a member of the AAA+ family of ATPases. This protein is encoded by the VCP gene. It is a mechanoenzyme that uses energy from ATP hydrolysis to promote protein unfolding and segregation actively.
Constanza Salinas-Rebolledo +17 more
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Proteolysis-Targeting Chimera (PROTAC): Is the Technology Looking at the Treatment of Brain Tumors? [PDF]
Frontiers in Cell and Developmental Biology, 2022 Post-translational modifications, such as ubiquitylation, need to be tightly controlled to guarantee the accurate localization and activity of proteins.
Ludovica Lospinoso Severini +4 more
doaj +4 more sources
Proteolysis‐Targeting Chimera (PROTAC): Current Applications and Future Directions [PDF]
MedCommTargeted protein degradation (TPD) represents a paradigm shift in drug discovery, moving beyond traditional binding‐based inhibition toward active removal of disease‐driving proteins.
Gang Fan +9 more
doaj +2 more sources
Highly efficient and long-acting split-and-mix proteolysis targeting chimera based on self-assembled polylactic acid [PDF]
Nature CommunicationsProteolysis targeting chimera (PROTAC) technology has received extensive attention due to its “event-driven” mechanism of action. However, existing chimera molecules tend to have higher molecular weight and higher polar surface area and exhibit lower ...
Mei-miao Zhan +12 more
doaj +2 more sources
Proteolysis-targeting Chimera efficacy prediction using a deep-learning–QSP model [PDF]
Journal of CheminformaticsThis study presents an integrated computational modeling framework combining deep learning and Quantitative Systems Pharmacology (QSP) to predict the efficacy of PROTAC (PROteolysis Targeting Chimera) molecules.
Sungwoo Goo +6 more
doaj +2 more sources
Discovery of a Proteolysis Targeting Chimera for TRKA and RET-derived oncoproteins [PDF]
Scientific ReportsWe designed Proteolysis Targeting Chimeras (PROTACs) to target Tropomyosin Receptor Kinase A (TRKA) and Rearranged during Transfection (RET) oncogenic proteins.
Marialuisa Moccia +7 more
doaj +2 more sources
Proteolysis-Targeting Chimera (PROTAC) Delivery into the Brain across the Blood-Brain Barrier [PDF]
Antibodies, 2023 Drug development for neurodegenerative diseases such as Alzheimer’s disease, Parkinson’s disease, and Huntington’s disease has challenging difficulties due to the pharmacokinetic impermeability based on the blood-brain barrier (BBB) as well as the ...
Toshihiko Tashima
doaj +2 more sources
A novel proteolysis-targeting chimera strategy targeting multiple immune checkpoints containing ITIMs enhances antitumor immunity [PDF]
Journal of Pharmaceutical AnalysisImmune checkpoint inhibitors (ICIs) have significantly advanced and revolutionized cancer treatment over the past decade; however, their clinical benefits have been limited to a subset of cancer patients.
Yue-Yuan Qiu +12 more
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
HSP70 Interactome‐Mediated Proteolysis Targeting Chimera (HSP70‐PROTAC) for Ferroptosis‐Driven Cancer Treatment [PDF]
Advanced ScienceTargeted protein degradation (TPD) represents a transformative therapeutic paradigm that harnesses the cellular degradation machinery to pharmacologically eliminate disease‐causing proteins with aberrant expression.
Jinyun Dong +15 more
doaj +2 more sources