The WEE1 tyrosine kinase is an important cell cycle regulator that inhibits cell cycle progression during the S and G2/M phases to impede the division of cells with DNA damage. Tumor cells with replicative stress are thought to rely on WEE1 for their survival.
Gluetacs Therapeutics (Shanghai) Co. Ltd. has synthesized molecular glue degraders comprising a cereblon (CRBN) binding moiety acting as protein degradation inducers reported to be useful for the treatment of anemia, cancer, diabetes, infections, transplant rejection, inflammation, autoimmune and sarcoidosis, among others.
BMS-986470 is a potentially first-in-class molecular glue dual degrader, targeting zinc finger and BTB domain containing 7A (ZBTB7A) and widely interspaced zinc finger protein (WIZ). Bristol Myers Squibb Inc. recently presented details on the discovery of BMS-986470, which is now in phase I studies for the treatment of sickle cell disease (SCD) (NCT06481306).
Seed Therapeutics Inc. has gained IND clearance from the U.S. FDA for ST-01156, a brain-penetrant RBM39 degrader. The clearance enables initiation of a first-in-human phase I trial in patients with advanced solid tumors and hematological malignancies, prioritizing biomarker-selected RBM39-dependent cancers. Dosing is expected to begin in the first quarter of next year.
Primelink Biotherapeutics (Shenzhen) Co. Ltd. has discovered molecular glue degraders acting as eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1) degradation inducers reported to be useful for the treatment of cancer.
Discoidin domain receptor tyrosine kinase 1 (DDR1) contributes to tumor progression by promoting the alignment and densification of collagen fibers within the extracellular matrix (ECM), thereby facilitating the development of an immune-excluded tumor microenvironment (TME).
Polycystic ovary syndrome is a common endocrine disorder in women of reproductive age and characterized by obesity, insulin resistance and renal injury.
Dana Farber Cancer Institute Inc. and Stanford University have patented new molecular glue degraders comprising cereblon (CRBN) binding moiety acting as casein kinase 1 isoform α and/or wee1-like protein kinase (Wee1) degradation inducers reported to be useful for the treatment of cancer.