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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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Kinase-impaired BTK mutations are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127

Covalent Modifiers

Therefore, understanding mechanisms by which acquired mutations in BTK confer drug resistance and developing new therapies to overcome resistance are critically important. We therefore set out to understand the nonenzymatic functions of BTK and explored targeted protein degradation to overcome the oncogenic scaffold function of mutant BTK.

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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. Arvinas and Pfizer are seeking to develop ARV-471 as the potential endocrine therapy of choice for patients and their physicians.

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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.,