Blueprint Medicines Corp. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a cyclin dependent kinase 2 (CDK2)-targeting moiety through a linker reported to be useful for the treatment of cancer.

Astrazeneca AB has synthesized proteolysis targeting chimera (PROTAC) compounds comprising a protein cereblon (CRBN) binding moiety covalently linked to an estrogen receptor α (ER-α)-targeting moiety through a linker reported to be useful for the treatment of breast cancer.

Researchers at Shanghai Haiyan Pharmaceutical Technology Co. Ltd. and Yangtze River Pharmaceutical Group have disclosed proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to a polycomb protein EED-targeting moiety through linkers; they are reported to be useful for the treatment of 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.

Protier Biotech Inc. has patented protein/nucleic acid degraders comprising cereblon (CRBN)-binding agents covalently bound to a eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1)-targeting moiety via linker.

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.