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

Covalent Modifiers

Covalent and noncovalent inhibitors of BTK have revolutionized the treatment of these cancers. Therefore, understanding mechanisms by which acquired mutations in BTK confer drug resistance and developing new therapies to overcome resistance are critically important.

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Attacking Cancers Using Novel Methods of Targeted Protein Degradation

SugarCone Biotech

Cancer cell viability was reduced by 50% - 80% after 7 days treatment in vitro, however only limited in vivo data was shown in this paper. Because Trf1 is degraded as part of the degradation of the internalized protein complex, these EGFR-bright cells become iron-starved and die as a consequence.

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Cell-based protein degrader assays for microplates | BMG LABTECH

BMG Labtech

Options for cell-based protein degrader assays Interest is growing in the use of targeted-protein degradation to induce the breakdown of disease-causing proteins after treatment with small molecule drugs.

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Antibody-drug conjugates payloads: then, now and next

Drug Target Review

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.

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Sygnature Discovery and UBE Corporation successfully identify potent SHP2 Degrader Compounds

Sygnature Discovery

Sygnature Discovery identifies potent SHP2 degrader compounds using its proprietary targeted protein degrader platform, CHARMED, in collaboration with Japanese specialty chemical company, UBE Corporation.

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Women in STEM with Juliet Williams

Drug Target Review

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 protein degraders – which are opportunities to change how we think about medicines. I’ve already had a number of ‘rocking chair’ moments in my career.

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Sosei Heptares and Captor Therapeutics Enter Strategic Technology Collaboration Focused on Targeted GPCR Degradation as Novel Approach for Drug Design

The Pharma Data

. Unique combination of novel technologies to enhance GPCR drug discovery and expand capabilities into wider drug target universe. Captor’s Optigradeä platform is focused on improving the selectivity and performance of first-generation degrader drugs. TOKYO and CAMBRIDGE, England , Dec.