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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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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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AI in Drug Discovery - A Highly Opinionated Literature Review (Part III)

Practical Cheminformatics

Property Prediction Machine Learning Methods for Small Data Challenges in Molecular Science [link] Practical guidelines for the use of gradient boosting for molecular property prediction [link] Application of message passing neural networks for molecular property prediction [link] Molecular Similarity Molecular Similarity: Theory, Applications, and (..)

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Drug Hunter Journal Club: March 2023

Drug Hunter

BCCov “A covalent BTK ternary complex compatible with targeted protein degradation” Nat. Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples. Get ahead now by requesting a trial. already a member?

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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. ’23: DCAF1, on CNS Degraders, and More appeared first on Drug Hunter.

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Molecules of the Month – June 2023

Drug Hunter

With the popular success of diabetes and weight-loss peptide drugs from Novo (e.g. vorasidenib – An oral first-in-class dual IDH1/IDH2 inhibitor with efficacy in Phase III trials for IDH-mutant grade 2 gliomas, discovered through structure-based drug design (SBDD) of a prior mIDH inhibitor, developed by Agios and Servier.