Plexium Inc. has described the efforts that led to the discovery of PLX-4545, an orally bioavailable molecular glue degrader of IKZF2 for the treatment of cancer that is currently undergoing evaluation in a phase I study in healthy volunteers.
At the recently concluded ACS Fall meeting, Bristol Myers Squibb Co. reported the discovery of potent orally bioavailable B-cell lymphoma 6 protein (BCL6) ligand-directed degraders (LDDs).
The nucleotide-binding oligomerization domain-like receptor pyrin domain containing 3 (NLRP3) inflammasome is an intracellular multiprotein complex that may be activated by exogenous or endogenous signals and is involved in the pathogenesis of several inflammatory disorders.
Both casein kinase 1α (CK1α) and zinc finger protein Helios (IKZF2) are among the targets most recently evaluated for the treatment of acute myeloid leukemia (AML). A growing number of molecules against these targets acting as degraders or inhibitors are actively being investigated.
Big pharma continues to invest heavily into molecular glue degraders. The latest deal has Eisai Co. Ltd. striking up a research collaboration that could bring Seed Therapeutics Inc. up to $1.5 billion in up-front and milestone payments. The two said they plan to discover, develop and commercialize MGDs for several undisclosed neurodegeneration and oncology targets.
Pinetree Therapeutics Inc. has entered into an exclusive option and global license agreement with Astrazeneca plc for a preclinical epidermal growth factor receptor (EGFR) degrader candidate.
Monte Rosa Therapeutics Inc. has submitted an IND application to the FDA for MRT-6160, a highly selective and orally bioavailable molecular glue degrader directed against VAV1 in development for systemic and neurological autoimmune diseases.
Sibylla Biotech SpA and the University of Texas MD Anderson Cancer Center have signed a strategic collaboration agreement to discover and develop novel small molecule folding interfering degraders (FIDs) for the treatment of cancer.
Scientists at the Institute of Cancer Research have generated a proteolysis targeting chimera (PROTAC) that successfully destroyed RIPK1 in cancer cells.
Amphista Therapeutics Ltd. has unveiled a new mechanism of action for the degradation of the emerging oncology target BRD9 that is differentiated from cereblon- or VHL-based PROTACs.
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