Multifaceted targeted protein degradation systems for different cellular compartments
Sign Up to like & getrecommendations! Published in 2022 at "BioEssays"
DOI: 10.1002/bies.202200008
Abstract: Selective protein degradation maintains cellular homeostasis, but this process is disrupted in many diseases. Targeted protein degradation (TPD) approaches, built upon existing cellular mechanisms, are promising methods for therapeutically regulating protein levels. Here, we review… read more here.
Keywords: cellular compartments; targeting chimeras; protein degradation; targeted protein ... See more keywords
Development of Integrin Targeting Chimeras (ITACs) for the Lysosomal Degradation of Extracellular Proteins
Sign Up to like & getrecommendations! Published in 2024 at "ChemMedChem"
DOI: 10.1002/cmdc.202300643
Abstract: The emerging of lysosomal targeting chimera (LYTAC) expands the field of targeted protein degradation (TPD) to include the extracellular proteins for precise depletion. However, most of the reported LYTACs either induce ubiquitous degradation of the… read more here.
Keywords: extracellular proteins; degradation; integrin; targeting chimeras ... See more keywords
Advancements in Proteolysis Targeting Chimeras for Targeted Therapeutic Strategies in Alzheimer’s Disease
Sign Up to like & getrecommendations! Published in 2025 at "Molecular Neurobiology"
DOI: 10.1007/s12035-025-04838-0
Abstract: The presence of hyperphosphorylated Tau proteins, which mislocalize and form neurofibrillary tangles, and the accumulation of amyloid-β plaques are hallmark features of Alzheimer’s disease (AD). These toxic protein aggregates contribute to synaptic impairment and neuronal… read more here.
Keywords: alzheimer disease; targeting chimeras; proteolysis targeting; chimeras targeted ... See more keywords
Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective.
Sign Up to like & getrecommendations! Published in 2020 at "Drug discovery today"
DOI: 10.1016/j.drudis.2020.07.013
Abstract: Proteolysis-targeting chimeras (PROTACs) are an emerging therapeutic modality with the potential to open target space not accessible to conventional small molecules via a degradation-based mechanism; however, their bifunctional nature can result in physicochemical properties that… read more here.
Keywords: metabolism pharmacokinetics; targeting chimeras; drug; proteolysis targeting ... See more keywords
Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.0c00793
Abstract: Hetero-bifunctional PROteolysis TArgeting Chimeras (PROTACs) represent a new emerging class of small molecules designed to induce polyubiquitylation and proteasomal-dependent degradation of a target protein. Despite the increasing number of publications about the synthesis, biological evaluation,… read more here.
Keywords: understanding metabolism; metabolism; targeting chimeras; proteolysis targeting ... See more keywords
Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00482
Abstract: A current bottleneck in the development of proteolysis targeting chimeras (PROTACs) is the empirical nature of linker length structure-activity relationships (SARs). A multidisciplinary approach to alleviate the bottleneck is detailed here. First, we examine four… read more here.
Keywords: linker design; targeting chimeras; chemistry; proteolysis targeting ... See more keywords
Rational Design for Nitroreductase (NTR)-Responsive Proteolysis Targeting Chimeras (PROTACs) Selectively Targeting Tumor Tissues.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02221
Abstract: The catalytic properties of proteolysis targeting chimeras (PROTACs) may lead to uncontrolled off-tissue target degradation that causes potential toxicity, limiting their clinical applications. The precise control of this technology in a tissue-selective manner can minimize… read more here.
Keywords: ntr responsive; chimeras protacs; proteolysis targeting; tumor tissues ... See more keywords
Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00345
Abstract: Several epidermal growth factor receptor (EGFR) proteolysis-targeting chimeras (PROTACs), including MS39 and MS154 developed by us, have been reported to effectively degrade the mutant but not the wild-type (WT) EGFR. However, the mechanism underlying the… read more here.
Keywords: epidermal growth; growth factor; mutant wild; egfr ... See more keywords
Deubiquitinase-Targeting Chimeras (DUBTACs) as a Potential Paradigm-Shifting Drug Discovery Approach.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c02975
Abstract: Developing proteolysis-targeting chimeras (PROTACs) is well recognized through target protein degradation (TPD) toward promising therapeutics. While a variety of diseases are driven by aberrant ubiquitination and degradation of critical proteins with protective functions, target protein… read more here.
Keywords: potential paradigm; targeting chimeras; chimeras dubtacs; dubtacs potential ... See more keywords
Targeted Degradation of Histone Deacetylases via Bypassing E3 Ligase Targeting Chimeras (BYETACs).
Sign Up to like & getrecommendations! Published in 2025 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.5c00193
Abstract: Targeted protein degradation (TPD) through heterobifunctional molecules to initiate ubiquitination and facilitate subsequent degradation has emerged as a powerful therapeutic strategy. Most heterobifunctional molecules designed for TPD function primarily through a limited set of E3… read more here.
Keywords: degradation; targeted degradation; targeting chimeras; histone deacetylases ... See more keywords
Indolequinone-Based Hypoxia-Activated Proteolysis Targeting Chimeras Selectively Degrade BRD4 in Hypoxic Cancer Cells
Sign Up to like & getrecommendations! Published in 2025 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.5c10240
Abstract: Proteolysis targeting chimeras (PROTACs) have helped to establish proximity induction as an exciting strategy in drug discovery, and there are multiple clinical trials focused on this modality. However, degradation of a full protein in a… read more here.
Keywords: targeting chimeras; hypoxia activated; group; proteolysis targeting ... See more keywords