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.
Oxford University Innovations Ltd. has synthesized hypoxia-activated proteolysis targeting chimeras (hypoxia-activated PROTACs; HAP-TAC) comprising a hypoxia-activated moiety modified E3 ubiquitin ligase-binding moiety coupled to a protein targeting moiety through a linker reported to be useful for the treatment of cancer.
Aurigene Oncology Ltd. has patented new proteolysis targeting chimera (PROTACs) compounds comprising a protein cereblon (CRBN)-binding moiety covalently bound to a CREB-binding protein (CREBBP; CBP)-targeting moiety through a linker.
Prelude Therapeutics Inc. described the discovery of PRT-3789, a first-in-human, highly potent and selective SMARCA2-targeted protein degrader, for the potential treatment of cancer.
At last week’s American Chemical Society Spring meeting, Bristol Myers Squibb Co. discussed the development of a potent, orally bioavailable and highly selective cereblon (CRBN)-mediated ligand-directed degrader (LDD) of B-cell lymphoma 6 protein (BCL6), BMS-986458, for the treatment of B-cell non-Hodgkin lymphoma.
Kymera Therapeutics Inc. has described proteolysis targeting chimera (PROTACs) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a signal transducer and activator of transcription 6 (STAT6)-targeting moiety.
Patents from Oncopia Therapeutics Inc. (dba SK Life Science Labs) describe proteolysis targeting chimeric (PROTACs) compounds reported to be useful for the treatment of cancer, autoimmune and inflammatory disorders.
A Bristol Myers Squibb Co. patent detailed new substituted phenyl oxooxazolyl piperidine dione molecular glue degraders acting as DNA-binding protein Ikaros (IKZF1), zinc finger protein Helios (IKZF2), Aiolos (IKZF3) and Eos (IKZF4) degradation inducers potentially useful for the treatment of cancer.
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