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This article highlights six recent articles of interest in the field of targetedproteindegradation 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.
Therefore, understanding mechanisms by which acquired mutations in BTK confer drug resistance and developing new therapies to overcome resistance are critically important. This effort included evaluation of BTK degradation in patients with CLL treated in a phase 1 clinical trial of NX-2127, a first-in-class BTK degrader (NCT04830137).
It is important to be clear that this is a unique degrader strategy and not at all like ProTAC or ProMAB technologies that targetsproteins by binding them to the E3-ligase controlled degradation pathway. That is a complex field that has struggled to bring therapies to approval (see [link] ).
In person Molecular glues and targetedproteindegraders are revolutionizing the field of drug discovery, offering promising solutions for a range of diseases, including cancer, infectious, inflammatory, and neurodegenerative diseases. The recent emergence of the molecular glue class of proteindegraders is paving.
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 targetedproteindegradation researchers, and brain-penetrant HER2 and ROCK2 inhibitors.
Antibody-drug conjugates (ADCs) have been a groundbreaking approach to cancer treatment with their ability to deliver cytotoxic drugs directly to diseased cells while sparing healthy tissues. 1 However, efforts proved less effective than the original drugs, owing mostly to insufficient toxicity against cancer cells.
In person Molecular glues and targetedproteindegraders are revolutionizing the field of drug discovery, offering promising solutions for a range of diseases, including cancer, infectious, inflammatory, and neurodegenerative diseases. The recent emergence of the molecular glue class of proteindegraders is paving.
In person Molecular glues and targetedproteindegraders are changing the landscape of drug discovery. They show great potential for treating diseases such as cancer, infectious, inflammatory, andneurodegenerative diseases, especially for those with “undruggable” pathogenic proteintargets.
In person Molecular glues and targetedproteindegraders are changing the landscape of drug discovery. They show great potential for treating diseases such as cancer, infectious, inflammatory, andneurodegenerative diseases, especially for those with “undruggable” pathogenic proteintargets.
This laid the groundwork for my career in drug discovery using novel modalities like small molecule inhibitors, antibodies, RNA interference (RNAi) and, currently, small molecule proteindegraders – which are opportunities to change how we think about medicines. I’ve already had a number of ‘rocking chair’ moments in my career.
This collaboration has the potential to be transformational, as it combines our leadership in targetedproteindegradation with Pfizer’s global capabilities and deep expertise in breast cancer. Arvinas and Pfizer are seeking to develop ARV-471 as the potential endocrine therapy of choice for patients and their physicians.
a leading biotechnology company developing small molecule therapeutics based on its proprietary uSMITE platform of targetedproteindegradation technology, today announced that the company’s internal program to develop selective degraders that target key proteins within the TRK family has been published by the Journal of Medicinal Chemistry.
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Monte Rosa Therapeutics has raised $96m in Series B financing to support further develop of its pipeline of small-molecule proteindegraders. The company, which was originally formed as a spinout from Cancer Research UK-funded research at the Institute of Cancer Research, specialises in targetedproteindegradation.
Nasdaq: ARVN), a clinical-stage biotechnology company creating a new class of drugs based on targetedproteindegradation 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.,
Over the two days, we’ll bring together academia, industry, and the vendor community to discuss recent advancements in two ultra-exciting areas of drug discovery and biological research: therapeutic oligonucleotides and chemical biology. Right now, targetedproteindegradation is a critical focus topic across both industry and academia.
Given this ever-increasing body of evidence, why is it that for so long, they have not been the focus of drug discovery? Lacking active sites entirely, transcription factors are instead largely regulated by post-translational modification, which in turn impacts changes in conformation, behavior, and interaction with other proteins.
As context, biotech business models have largely had two flavors for decades: asset-centric investments focused on specific product opportunities and platforms (discovery engines) designed to create new drugs based on novel modalities, technologies, or biological insights. In each moment, we’ve seen a reversion to asset incrementalism (e.g.,
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