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Home » Topics » Drugs » Degradation inducer

Degradation inducer
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Cancer

Prelude Therapeutics describes new SMARCA2 and SMARCA4 degradation inducers

June 4, 2025
Prelude Therapeutics Inc. has described proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase binding moiety covalently linked to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety through a linker. They are reported to be useful for the treatment of cancer.
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Cancer

Bcl-xl degradation inducers disclosed in Treeline patents

June 2, 2025
Treeline Biosciences Inc. has divulged proteolysis targeting chimeras (PROTACs) comprising cereblon (CRBN) ligands coupled to a Bcl-2-like protein 1 (Bcl-xl; Bcl-X; BCL2L1) targeting moiety via a linker acting as Bcl-xl degradation inducers reported to be useful for the treatment of cancer.
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Doctor points at molecular structure
Cancer

Chinese researchers describe first-in-class PRMT1 degrader

May 30, 2025
No Comments
PRMT1 is a key enzyme that catalyzes asymmetric dimethylation of arginine residues and overexpressed in various cancers and inflammatory diseases. While current PRMT1 inhibitors lack specificity and effectiveness, targeted degradation of PRMT1 offers a potential strategy to treat PRMT1-driven conditions and explore its nonenzymatic roles.
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Cancer

Bpgbio divulges new ESR1 degradation inducers

May 27, 2025
Bpgbio Inc. has synthesized bifunctional compounds comprising an E2 ubiquitin ligase binding ligand covalently linked to an estrogen receptor α (ER-α; ESR1) targeting moiety through a linker acting as ESR1 degradation inducers reported to be useful for the treatment of cancer.
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Pipet, test tubes, chemical structures
Cancer

A structural scaffold for protein degraders against multiple myeloma

May 26, 2025
No Comments
In their efforts to develop next-generation drugs whose structures differ from those of conventional IMiDs, researchers at Fujimoto Pharmaceutical Corp. developed FPFT-2216 through optimization of a lead compound.
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Respiratory

KT-621: a first-in-class STAT6 degrader for Th2-driven diseases

May 22, 2025
No Comments
STAT6 plays a central role in regulating Th2-driven immune responses. Recent studies have identified gain-of-function mutations in the STAT6 gene that are associated with early-onset, severe allergic diseases. As a result, STAT6 has emerged as a promising therapeutic target in conditions such as asthma, eosinophilic inflammation, food allergies and atopic dermatitis, particularly in cases that are refractory to standard therapies.
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Cancer

Chinese researchers unveil new agent for KRAS G12D-mutated tumors

May 13, 2025
No Comments
The KRAS G12D mutation is the most common oncogenic KRAS variant, identified in approximately 34% of pancreatic ductal adenocarcinoma cases, 12% of colorectal cancers and 4% of lung adenocarcinomas.
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Cancer

Chinese researchers unveil new agent for KRAS G12D-mutated tumors

May 9, 2025
No Comments
The KRAS G12D mutation is the most common oncogenic KRAS variant, identified in approximately 34% of pancreatic ductal adenocarcinoma cases, 12% of colorectal cancers and 4% of lung adenocarcinomas.
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Cancer

Novel PROTAC shows robust antitumor activity in preclinical models of prostate cancer

May 6, 2025
No Comments
Researchers from Jiangsu Hengrui Pharmaceuticals Co. Ltd. reported the discovery of SHR-3591, an orally bioavailable AR proteolysis targeting chimera (PROTAC) designed to treat prostate tumors.
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Illustration of triple-negative breast cancer cells
Cancer

A high-affinity small-molecule inhibitor of STAT3 against triple-negative breast cancer

May 2, 2025
No Comments
Triple-negative breast cancer (TNBC), which accounts for up to 20% of cases of breast cancer, is one of the most aggressive and difficult to treat subtypes of the disease.
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