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
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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
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Proteolysis Targeting Chimera Loaded Extracellular Vesicles for Developing Triple Negative Breast Cancer Treatment [PDF]
Journal of Extracellular VesiclesProteolysis targeting chimeras (PROTACs) represent an emerging targeted cancer therapy approach. However, their poor cell penetration and instability in vivo pose daunting challenges for wide‐spread clinical usage.
Nina Erwin +11 more
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Proteolysis targeting chimera (PROTAC)-driven antibody internalization of oncogenic cell surface receptors [PDF]
Communications BiologyAntibody-drug conjugates (ADCs) are increasingly used in clinic for multiple indications and may improve upon the activity of parental antibodies by delivering cytotoxic payloads into target cells.
Ezequiel J. Tolosa +9 more
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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
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Proteolysis-targeting chimeras with reduced off-targets [PDF]
Nature Chemistry, 2021 ABSTRACT Proteolysis Targeting Chimeras (PROTACs), a class of heterobifunctional molecules that recruit target proteins to E3 ligases, have gained traction for targeted protein degradation. However, pomalidomide, a widely used E3 ligase recruiter in PROTACs, can independently degrade other targets, such as zinc-finger (ZF) proteins ...
Tuan M. Nguyen +15 more
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Crizotinib‐based proteolysis targeting chimera suppresses gastric cancer by promoting MET degradation [PDF]
Cancer Science, 2023 Xin Luan
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Proteolysis-targeting chimeras and their implications in breast cancer [PDF]
Exploration of Targeted Anti-tumor Therapy, 2021 Breast cancer (BC) is a highly heterogeneous neoplasm of the mammary tissue, causing the deaths of a large number of women worldwide. Nearly 70% and 20% of BC cases are estrogen receptor alpha positive (ERα+) and human epidermal growth factor receptor 2-positive (HER2+), respectively; therefore, ER and HER2 targeted therapies have been employed in BC ...
Angeles C. Tecalco-Cruz +3 more
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Molecular Strategies to Target Protein Aggregation in Huntington’s Disease
Frontiers in Molecular Biosciences, 2021 Huntington’s disease (HD) is a neurodegenerative disorder caused by the aggregation of the mutant huntingtin (mHTT) protein in nerve cells. mHTT self-aggregates to form soluble oligomers and insoluble fibrils, which interfere in a number of key cellular ...
Olga D. Jarosińska +3 more
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Proteolysis-targeting chimera (PROTAC) delivery system: advancing protein degraders towards clinical translation [PDF]
Chemical Society Reviews, 2022 Ira Tandon, William J Heelan, Yixin Wang
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