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   Articles with "based protacs" as a keyword



Developments of CRBN-based PROTACs as potential therapeutic agents.

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recommendations! Published in 2021 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2021.113749

Abstract: Protease-targeted chimeras (PROTACs) are a new technology that is receiving much attention in the treatment of diseases. The mechanism is to inhibit protein function by hijacking the ubiquitin E3 ligase for protein degradation. Heterogeneous bifunctional… read more here.

Keywords: based protacs; crbn based; developments crbn; protacs potential ... See more keywords

Indomethacin-based PROTACs as pan-coronavirus antiviral agents

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recommendations! Published in 2021 at "European Journal of Medicinal Chemistry"

DOI: 10.1016/j.ejmech.2021.113814

Abstract: Indomethacin (INM), a well-known non-steroidal anti-inflammatory drug, has recently gained attention for its antiviral activity demonstrated in drug repurposing studies against severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). Although the mechanism of action of INM is… read more here.

Keywords: based protacs; pan coronavirus; inm; protacs ... See more keywords

Phosphorothioate-Modified DNA Aptamer-Based PROTACs for Targeted Degradation of Estrogen Receptor α.

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recommendations! Published in 2025 at "Bioconjugate chemistry"

DOI: 10.1021/acs.bioconjchem.5c00242

Abstract: Proteolysis-targeting chimeras (PROTACs) have emerged as a powerful modality for selectively degrading intracellular proteins via the ubiquitin-proteasome system. However, their development is often hindered by the limited availability of high-affinity small-molecule ligands, particularly for challenging… read more here.

Keywords: chemistry; based protacs; degradation; aptamer based ... See more keywords
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Persistent Degradation of HER2 Protein by Hybrid nanoPROTAC for Programmed Cell Death.

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recommendations! Published in 2023 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.3c00013

Abstract: Proteolysis-targeting chimera (PROTAC) has emerged as a promising strategy for degrading proteins of interest. Peptide-based PROTACs offer several advantages over small-molecule-based PROTACs, such as high specificity, low toxicity, and large protein-protein interaction surfaces. However, peptide-based… read more here.

Keywords: peptide based; cell; her2; based protacs ... See more keywords

Bumped pomalidomide-based PROTACs

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recommendations! Published in 2024 at "Communications Chemistry"

DOI: 10.1038/s42004-024-01125-2

Abstract: Pomalidomide is an E3 ligase recruiter exploited by PROTACs to degrade target proteins, but its application is hampered by the off-target degradation of other vital endogenous zinc finger (ZF) proteins. Now, the off-target ZF binding… read more here.

Keywords: chemistry; based protacs; bumped pomalidomide; target ... See more keywords

Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs

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recommendations! Published in 2025 at "Communications Chemistry"

DOI: 10.1038/s42004-025-01598-9

Abstract: PROteolysis-Targeting Chimeras (PROTACs) are an emerging class of molecules capable of inducing a forced approximation between a protein of interest (POI) and an E3 ligase enzyme (e.g., Cereblon), leading to the degradation of the POI… read more here.

Keywords: based protacs; synthesis; clinical trials; cereblon based ... See more keywords

Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents

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recommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"

DOI: 10.1080/14756366.2022.2074414

Abstract: Abstract Proteolytic targeting chimaeras (PROTACs) have been developed as an effective technology for targeted protein degradation. PROTACs are heterobifunctional molecules that can trigger the polyubiquitination of proteins of interest (POIs) by recruiting the ubiquitin-proteasome system,… read more here.

Keywords: protacs; advances iap; based protacs; therapeutic agents ... See more keywords

Peptide-based PROTACs: Current Challenges and Future Perspectives.

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recommendations! Published in 2023 at "Current medicinal chemistry"

DOI: 10.2174/0929867330666230130121822

Abstract: Proteolysis-targeting chimeras (PROTACs) are an attractive means to target previously undruggable or drug-resistant mutant proteins. While small molecule-based PROTACs are stable and can cross cell membranes, there is limited availability of suitable small molecule warheads… read more here.

Keywords: peptide based; small molecule; protacs current; based protacs ... See more keywords