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.
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.
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.
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.
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.
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.
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.
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.
Targeted protein degradation has yet to notch its first approval. But with more than two dozen agents now in clinical trials, the strategy’s ultimate clinical validation appears to be a matter of time.
SMARCA4 and SMARCA2 are essential subunits of the SWI/SNF complex, functioning as ATP-dependent chromatin remodelers that regulate gene expression and maintain cellular homeostasis. Recent research has shown that selectively targeting SMARCA2 is an effective cancer treatment strategy, with several compounds already in early clinical testing.
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