PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
Exploration of Targeted Anti-tumor Therapy, 2020 BCL-XL is an anti-apoptotic protein that plays an important role in tumorigenesis, metastasis, and intrinsic or therapy-induced cancer drug resistance.
Peiyi Zhang +5 more
doaj +1 more source
Proteolysis targeting chimeras (PROTACs) in cancer therapy [PDF]
Journal of Experimental & Clinical Cancer Research, 2020 AbstractExploitation of the protein degradation machinery as a therapeutic strategy to degrade oncogenic proteins is experiencing revolutionary advances with the development of proteolysis targeting chimeras (PROTACs). PROTACs are heterobifunctional structures consisting of a ligand that binds a protein to be degraded and a ligand for an E3 ubiquitin ...
Alberto Ocaña, Atanasio Pandiella
openaire +5 more sources
, 2022 Lactate dehydrogenase (LDH) is a key glycolytic enzyme and biomarker of aggressive cancers. LDHA and LDHB are two main LDH subunits, and both are frequently overexpressed in tumors and essential for tumor growth.
Xiaoping Hu (231981) +8 more
core +2 more sources
Data for: Discovery of Potent Proteolysis Targeting Chimera Degrader of IDO1
, 2020 Supplementary Information for Discovery of Potent Proteolysis Targeting Chimera Degrader of ...
Yongmei Xie (5162336) +10 more
core +1 more source
Research advances in targeted protein degradation technologies [PDF]
Yixue xinzhi zazhiTargeted protein degradation (TPD) technologies leverage the body’s innate protein degradation systems to selectively eliminate protein of interest (POI).
PI Chuan +4 more
doaj +1 more source
, 2022 Enhancer of zeste homolog 2 (EZH2), a catalytic subunit of polycomb repressive complex 2 (PRC2), is overexpressed in triple-negative breast cancer (TNBC), correlating with poor prognosis.
Chengwei Zhang (573927) +10 more
core +2 more sources
Design, synthesis, and biological characterization of proteolysis targeting chimera (PROTACs) for the Ataxia telangiectasia and RAD3-related (ATR) kinase [PDF]
The Ataxia telangiectasia and RAD3-related (ATR) kinase is a key regulator of DNA replication stress responses and DNA-damage checkpoints. Several potent and selective ATR inhibitors are reported and four of them are currently in clinical trials in ...
Anne-Christin, Sarnow +7 more
core +3 more sources
Assays and Technologies for Developing Proteolysis Targeting Chimera Degraders [PDF]
Future Medicinal Chemistry, 2020 Targeted protein degradation by small-molecule degraders represents an emerging mode of action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules that can recruit an E3 ligase and a protein of interest (POI) into proximity, leading to induced ubiquitination and degradation of the POI by the proteasome system.
Xingui Liu +5 more
openaire +2 more sources
A Mathematical Model for Covalent Proteolysis Targeting Chimeras: Thermodynamics and Kinetics underlying Catalytic Efficiency [PDF]
, 2021 Proteolysis targeting chimeras (PROTACs), heterobifunctional protein degraders, have emerged as an exciting and transformative technology in chemical biology and drug discovery to degrade disease-causing proteins through co-opting of the ubiquitin ...
Charu, Chaudhry
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Development of KEAP1-targeting PROTAC and its antioxidant properties: In vitro and in vivo
Redox Biology, 2023 Oxidative stress due to abnormal accumulation of reactive oxygen species (ROS) is an initiator of a large number of human diseases, and thus, the elimination and prevention of excessive ROS are important aspects of preventing the development of such ...
Se Yong Park +10 more
doaj +1 more source