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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.
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] ).
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.
This approach showcases the potential of nucleophilic amino acid labeling probes, particularly for proteins lacking easily accessible cysteine residues, opening new possibilities for covalent PROTAC design and targetedproteindegradationtherapies.
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 targetedproteindegradation to overcome the oncogenic scaffold function of mutant BTK.
Dual payload ADCs As effective as therapies have been in treating solid and haematological cancers, tumour heterogeneity and resistance remain major clinical challenges. To overcome these obstacles, combination therapy, which delivers multiple small molecules, has emerged as a potential solution. 1 , 33–43 (2018). 102 , 1–6 (2016).
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 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.
Focusing on my time as Head of Research at Kymera, I’ve been fortunate to break new ground in drug discovery and development by advancing the science of targetedproteindegradation (TPD) and progressing an industry leading pipeline to solve critical health problems that traditional medicines cannot address.
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.,
Amgen is a proud sponsor of MBC BioLabs, assisting high-potential and innovative early-stage life science and biotech companies accelerating development of new therapies to improve human health. We look forward to interacting with Amgen ‘s scientific and therapeutic experts to help move Trilomer® therapies into the clinic.
Right now, targetedproteindegradation is a critical focus topic across both industry and academia. All the techniques being discussed have profound consequences for future therapies, so the talks will be immensely valuable,” said Dr Herzog.
During this time, novel science-heavy platforms were “hot” and well-funded: CRISPR, gene therapy, CAR-T, TargetedProteinDegradation, oligo/mRNAs, next gen chemistry, ADCs, Radiopharm, bispecifics… Truly an amazing period, and Atlas started and backed a number of great stories during this period (e.g.,
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