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   Articles with "targeting chimeras" as a keyword



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Multifaceted targeted protein degradation systems for different cellular compartments

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recommendations! 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
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Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective.

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recommendations! 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
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Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications

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recommendations! 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
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Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras.

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recommendations! 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
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Rational Design for Nitroreductase (NTR)-Responsive Proteolysis Targeting Chimeras (PROTACs) Selectively Targeting Tumor Tissues.

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recommendations! 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
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Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras.

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recommendations! 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

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

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recommendations! Published in 2020 at "Oncogene"

DOI: 10.1038/s41388-020-1336-y

Abstract: Using PROteolysis TArgeting Chimeras (PROTACs) to degrade proteins that are important for tumorigenesis has emerged as a potential therapeutic strategy for cancer. PROTACs are heterobifunctional molecules consisting of one ligand for binding to a protein… read more here.

Keywords: anticancer therapeutics; targeting chimeras; proteolysis targeting; protacs ... See more keywords
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Hypoxia deactivates epigenetic feedbacks via enzyme-derived clicking proteolysis-targeting chimeras

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recommendations! Published in 2022 at "Science Advances"

DOI: 10.1126/sciadv.abq2216

Abstract: Epigenetic mediation through bromodomain and extraterminal (BET) proteins have progressively translated protein imbalance into effective cancer treatment. Perturbation of druggable BET proteins through proteolysis-targeting chimeras (PROTACs) has recently contributed to the discovery of effective therapeutics.… read more here.

Keywords: derived clicking; hypoxia deactivates; enzyme; enzyme derived ... See more keywords
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Abstract LB002: Extracellular vesicle loading of proteolysis targeting chimeras for targeted therapeutic delivery

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recommendations! Published in 2023 at "Cancer Research"

DOI: 10.1158/1538-7445.am2023-lb002

Abstract: Breast cancer is a significant public health issue that remains the second leading cause of cancer death among women. Current treatment strategies for breast cancer can contribute to severe side effects and insufficient efficacy. For… read more here.

Keywords: targeting chimeras; protac; proteolysis targeting; delivery ... See more keywords
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Proteolysis-targeting chimeras (PROTACs) in cancer therapy

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recommendations! Published in 2022 at "Molecular Cancer"

DOI: 10.1186/s12943-021-01434-3

Abstract: Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits target protein and E3 ubiquitin ligase together to trigger proteasomal degradation of target protein by the… read more here.

Keywords: targeting chimeras; cancer; protacs; proteolysis targeting ... See more keywords
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Major Advances in Emerging Degrader Technologies

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recommendations! Published in 2022 at "Frontiers in Cell and Developmental Biology"

DOI: 10.3389/fcell.2022.921958

Abstract: Recently, degrader technologies have attracted increasing interest in the academic field and the pharmaceuticals industry. As one of the degrader technologies, proteolysis-targeting chimeras (PROTACs) have emerged as an attractive pharmaceutical development approach due to their… read more here.

Keywords: major advances; degrader technologies; protacs; advances emerging ... See more keywords