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
doaj +4 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 +3 more sources
Design, Synthesis and Biological Evaluation of α-Synuclein Proteolysis-Targeting Chimeras
Molecules, 2023 α-Synuclein aggregation under pathological conditions is one of the causes of related neurodegenerative diseases. PROTACs (proteolysis targeting chimeras) are bifunctional small molecules that induce a post-translational erasure of proteins via the ...
Jiyan Pang, Tianzhi Wen
exaly +3 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
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
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
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) in cancer: design principles and applications on “undruggable” targets [PDF]
Biomarker ResearchTargeted cancer therapies can enhance in vivo efficacy and decrease side effects by changing the distribution and exposure of specific biomolecules in tissues.
Xun Lu +9 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