Betta Pharmaceuticals Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising a VHL-binding agent coupled to a GTPase KRAS-targeting moiety through a linker acting as KRAS degradation inducers reported to be useful for the treatment of cancer.
Monte Rosa Therapeutics Inc. has gained IND clearance from the FDA for MRT-8102, a NEK7-directed molecular glue degrader being developed to treat inflammatory conditions linked to NLRP3, IL-1β and IL-6 dysregulation.
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.
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.
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