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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.

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Attacking Cancers Using Novel Methods of Targeted Protein Degradation

SugarCone Biotech

It is important to be clear that this is a unique degrader strategy and not at all like ProTAC or ProMAB technologies that targets proteins 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] ).

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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.

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Oncology Market Outlook 2024

Fierce BioTech

It addresses CAR-T therapies, KRAS, radiopharmaceuticals, & targeted protein degradation. It addresses CAR-T therapies, KRAS, radiopharmaceuticals, & targeted protein degradation. Blue Matter Consulting Resource Type Whitepaper BlueMatterConsulting_250x190 (1) (2).png

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Covalent PROTAC design method based on a sulfonyl pyridone probe

Covalent Modifiers

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 targeted protein degradation therapies.

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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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Antibody-drug conjugates payloads: then, now and next

Drug Target Review

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).