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   Articles with "chimeras protacs" as a keyword



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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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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

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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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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MDM2-Based Proteolysis-Targeting Chimeras (PROTACs): An Innovative Drug Strategy for Cancer Treatment

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recommendations! Published in 2022 at "International Journal of Molecular Sciences"

DOI: 10.3390/ijms231911068

Abstract: Proteolysis-targeting chimeras (PROTACs) are molecules that selectively degrade a protein of interest (POI). The incorporation of ligands that recruit mouse double minute 2 (MDM2) into PROTACs, forming the so-called MDM2-based PROTACs, has shown promise in… read more here.

Keywords: chimeras protacs; mdm2 based; proteolysis targeting; cancer treatment ... See more keywords

Proteolysis-Targeting Chimeras (PROTACs) in Cancer Therapy: Present and Future

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recommendations! Published in 2022 at "Molecules"

DOI: 10.3390/molecules27248828

Abstract: The PROteolysis TArgeting Chimeras (PROTACs) is an innovative technique for the selective degradation of target proteins via the ubiquitin–proteasome system. Compared with traditional protein inhibitor drugs, PROTACs exhibit advantages in the efficacy and selectivity of… read more here.

Keywords: chimeras protacs; cancer therapy; proteolysis targeting; targeting chimeras ... See more keywords