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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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Molecules of the Month – June 2023

Drug Hunter

danuglipron – An oral GLP-1-RA full agonist in Phase IIb clinical trials for obesity and Phase II trials for type 2 diabetes mellitus, identified through sensitized cell high-throughput screening and optimization, originated from Pfizer. Request a trial to check out substructure search and more features. Not 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. Get ahead now by requesting a trial. already a member?

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Patent Highlights: Allosteric AR Modulators, Glycogen Synthase Inhibitors, and More

Drug Hunter

This edition includes Maze’s glycogen synthase 1 (GYS1) inhibitors that were recently licensed to Sanofi, allosteric androgen receptor (AR) modulators that may be of interest to targeted protein degradation researchers, and brain-penetrant HER2 and ROCK2 inhibitors. Get ahead now by requesting a trial. already a member?

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ARVINAS AND PFIZER ANNOUNCE GLOBAL COLLABORATION TO DEVELOP AND COMMERCIALIZE PROTAC® PROTEIN DEGRADER ARV-471

The Pharma Data

(NYSE: PFE) today announced a global collaboration to develop and commercialize ARV-471, an investigational oral PROTAC® (PROteolysis TArgeting Chimera) estrogen receptor protein degrader. The estrogen receptor is a well-known disease driver in most breast cancers. Chief Executive Officer at Arvinas.

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How to Get Drugs Into the Brain

Drug Hunter

Obtaining adequate drug exposure in the brain is key to treating CNS diseases effectively. Prodrugs Remain in “Proof-of-Concept” Stages Prodrug strategies for CNS deliver have also been applied with varying success , with the most famous example being L-Dopa for Parkinson’s disease. What is K p,uu ? Figure 18.

Drugs 206
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Arvinas, Inc. Announces Pricing of $400 Million Public Offering of Common Stock

The Pharma Data

Nasdaq: ARVN), a clinical-stage biotechnology company creating a new class of drugs based on targeted protein degradation using its PROTAC ® Discovery Engine, today announced the pricing of an underwritten public offering of 5,714,286 shares of its common stock at a price of $70.00 NEW HAVEN, Conn.,