Genetic or pharmacologic inhibition of casein kinase 1α (CK1α) has proven effective in suppressing the proliferation of acute myeloid leukemia (AML) cell lines with wild-type TP53. Researchers from Bristol Myers Squibb Co. recently presented the discovery and preclinical characterization of BMS-986397, a cereblon E3 ligase modulatory drug (CELMoD) designed as a molecular glue degrader of CK1α.
Researchers from the UK Dementia Research Institute at the University of Cambridge have found how to prevent and reverse tau aggregation using target-specific nanobodies. The team holds great expertise in the role of TRIM21 in the tau environment since William McEwan, senior author of the study, first discovered TRIM21 and, a bit later, defined its contribution to tau immunotherapy efficacy.
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.
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