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.
Genentech Inc. has disclosed molecular glue compounds with the ability to induce cyclin-dependent kinase 2 (CDK2)/protein cereblon (CRBN) interaction for CDK2 degradation reported to be useful for the treatment of cancer.
Researchers from Captor Therapeutics Inc. presented the preclinical characterization of CT-01, a first-in-class GSPT-1 targeted degrader under investigation for the treatment of hepatocellular carcinoma.
Targeted protein degradation (TPD) is an alternative to conventional protein inhibition that is gaining attention due to advantages such as ensuring complete elimination of the target protein, reduced off-target effects or the potential to target previously inaccessible or “undruggable” proteins. Proteolysis targeting chimeras (PROTACs) are agents used for TPD that have proven effective for degradation of histone deacetylase (HDAC), among other different proteins.
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