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Exploiting the Cullin E3 Ligase Adaptor Protein SKP1 for Targeted Protein Degradation

Covalent Modifiers

Nomura ACS Chemical Biology 2024 DOI: [link] Targeted protein degradation with proteolysis targeting chimeras (PROTACs) is a powerful therapeutic modality for eliminating disease-causing proteins through targeted ubiquitination and proteasome-mediated degradation. Huang, Ingrid E.

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Covalency in PROTACs: Mechanisms and applications [@RPNowak]

Covalent Modifiers

Nowak Annual Reports in Medicinal Chemistry , 2024 [link] Proteolysis targeting chimeras (PROTACs) are hetero-bifunctional molecules that remove disease-causing proteins through the means of targeted protein degradation (TPD).

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Exploiting the Cullin E3 Ligase Adaptor Protein SKP1 for Targeted Protein Degradation

Covalent Modifiers

Seong Ho Hong , Akane Osa , Ingrid E Wertz , Daniel Nomura bioRxiv 2023.10.20.563371; doi: [link] Targeted protein degradation with Proteolysis Targeting Chimeras (PROTACs) is a powerful therapeutic modality for eliminating disease-causing proteins through targeted ubiquitination and proteasome-mediated degradation.

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Scientists generate new targeted protein degradation system that tunes a cell’s own proteins

Broad Institute

Related groups Liu lab Choudhary lab Fischer lab Researchers studying the role of proteins in health and disease use experimental tools that inactivate proteins, destroy them, or prevent them from being made in cells.

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Targeted protein degradation: turning undruggable targets into druggable targets

Drug Target Review

TPD is a rapidly evolving therapeutic modality to degrade a disease-causing proteins, thereby eliminating their function specifically. 1 TPD is expected to challenge undruggable proteins, which are highly difficult to target by conventional small molecules. How does TPD work? Nature News.

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Recruitment of FBXO22 for targeted degradation of NSD2 [@CherylArrowsmi1]

Covalent Modifiers

link] Targeted protein degradation (TPD) is an emerging therapeutic strategy that would benefit from new chemical entities with which to recruit a wider variety of ubiquitin E3 ligases to target proteins for proteasomal degradation. Tabor, J.R., Nat Chem Biol (2024).

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Degrader Radar, Apr. ’23: DCAF1, on CNS Degraders, and More

Drug Hunter

This article highlights six recent articles of interest in the field of targeted protein degradation including but not limited to potentially new ligases, recruiting motifs, and a discussion on the feasibility of CNS-penetrant degraders.