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): Is the Technology Looking at the Treatment of Brain Tumors?
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
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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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Telomerase reverse transcriptase degradation via a rationally designed covalent proteolysis targeting chimera. [PDF]
Bioorg Med Chem LettExpression of telomerase reverse transcriptase (TERT) is a hallmark of cancer, maintaining telomere length and integrity to enable replicative immortality.
Frost GB, Liu Y, Kron SJ, Scheidt KA.
europepmc +4 more sources
Proteolysis Targeting Chimeras in Antiviral Research
Future Medicinal Chemistry, 2022 An editorial on the role of PROTACs in antiviral ...
Desantis, Jenny, Goracci, Laura
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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 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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Self-Assembly of Proteolysis Targeting Chimeras Via Reversible Bioorthogonal Reactions [PDF]
, 2022 Targeted protein degradation (TPD) by PROteolysis TArgeting Chimeras (PROTACs) is of great interest for probe molecule and drug development. However, current bivalent PROTACs are rule-breaking molecules with sub-optimal cellular permeability, solubility,
Madeline, Balzarini +4 more
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Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers
Nature Communications, 2022 SMARCA2 has been identified as a synthetic lethal target in SMARCA4 mutated tumors, however, homology between the two has hindered the development of selective SMARCA2 inhibitors.
Jennifer Cantley +28 more
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