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Recent Highlights in Targeted Protein Degradation

Drug Hunter

In Wednesday’s Flash Talk webinar , we covered recent highlights in targeted protein degradation, with lots of great questions from the audience. KT-333 and KT-003) AR degraders and ER degraders from Arvinas (bavdegalutamide/ARV-110, ARV-766, and ARV-471) MDM2 degraders from Kymera (e.g.

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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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The Roles of Degrons in Targeted Protein Degradation | BMG LABTECH

BMG Labtech

At the most fundamental level you can think of a degron as a sequence of amino acids or a structural motif that can facilitate the degradation of protein substrates.

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Genentech takes up a deal to make ‘molecular glue’ drugs

BioPharma Drive: Drug Pricing

Targeted protein degradation has emerged as one of the more competitive areas of pharmaceutical research in recent years as scientists develop new ways to reach difficult-to-drug targets.

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

Broad Institute

It’s a big goal in biology to study loss of proteins under endogenous regulatory control, not only for validating drug targets, but also for studying native protein function in biology.” They then used prime editing to insert SD40 into the genome of human cells and tag two different proteins.

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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?

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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).