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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

With the popular success of diabetes and weight-loss peptide drugs from Novo (e.g. semaglutide/Ozempic), this month features a pair of ultra-hot non-peptide oral GLP-1R modulators in clinical development. Request a trial to check out substructure search and more features. Not 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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How to Get Drugs Into the Brain

Drug Hunter

Obtaining adequate drug exposure in the brain is key to treating CNS diseases effectively. Recently, Dennis Koester gave us a crash course in CNS drug discovery in a Drug Hunter Flash Talk. Why Kp,uu is the Most Important Parameter in CNS Drug Discovery What Influences the Kp,uu of Drugs?

Drugs 206
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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. Terms of the Collaboration.

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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.,