Researchers from the National Cancer Institute and their collaborators have presented data regarding a MLK3-degrading PROTAC, CEP1347-VHL-02, for treating triple-negative breast cancer.
B-cell lymphoma represents about 85% of non-Hodgkin lymphoma cases; therapeutic approaches are represented by Bruton tyrosine kinase (BTK) inhibitors, but still some issues, such as drug resistance and off-target toxicity, limit the clinical benefits.
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.
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