Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery [PDF]
Cell, 2020 New biological tools provide new techniques to probe fundamental biological processes. Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which are capable of modulating protein concentrations at a post-translational level by co-opting the ubiquitin-proteasome system. We describe the PROTAC technology and its application
George M, Burslem, Craig M, Crews
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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
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Caspase-7 uses an exosite to promote poly(ADP ribose) polymerase 1 proteolysis [PDF]
, 2012 During apoptosis, hundreds of proteins are cleaved by caspases, most of them by the executioner caspase-3. However, caspase-7, which shares the same substrate primary sequence preference as caspase-3, is better at cleaving poly(ADP ribose) polymerase 1 ...
Blais, Véronique +2 more
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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
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Minimal requirements for ubiquitination mediated regulation of thyroid hormone activation [PDF]
, 2014 Activation of thyroxine by outer ring deiodination is the crucial first step of thyroid hormone action. Substrate-induced ubiquitination of type 2 deiodinase (D2) is the most rapid and sensitive mechanism known to regulate thyroid hormone activation ...
Egri, Péter, Gereben, Balázs
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Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy
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
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BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design [PDF]
, 2019 Targeting subunits of BAF/PBAF chromatin remodeling complexes has been proposed as an approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera (PROTAC) degraders of the BAF ATPase subunits SMARCA2 and SMARCA4 using a ...
Arnhof, Heribert +36 more
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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
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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
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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
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