Prelude Therapeutics Inc. has prepared and tested new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and SMARCA4-targeting moiety through a linker.
Eubulus Biotherapeutics Inc. has identified molecular glue degraders acting as cyclin-dependent kinase 2 (CDK2) degradation inducers reported to be useful for the treatment of cancer.
Amphista Therapeutics Ltd. has released first data on its SMARCA2 program. The company conducted structurally guided discovery using high-resolution cryo-EM to deliver potent DCAF16-dependent Targeted Glues of SMARCA2, with exquisite selectivity over the closely related homologue SMARCA4.
In its second deal with Novartis AG of the past 11 months, Monte Rosa Therapeutics Inc. is getting $120 million up front to collaborate on developing molecular glue degraders to treat immune-mediated diseases. The agreement could swell to $5.7 billion for Monte Rosa.
Recurium IP Holdings LLC has patented new Wee1-like protein kinase (Wee1) inhibitors and/or degradation inducers reported to be useful for the treatment of cancer.
Hangzhou Polymed Biopharmaceuticals Inc. has identified proteolysis targeting chimera (PROTAC) compounds comprising a Von Hippel-Lindau disease tumor suppressor (VHL) ligase binding moiety covalently linked to a GTPase KRAS (G12D mutant) targeting moiety via a linker reported to be useful for the treatment of cancer.
Biogen Inc.’s IND application for BIIB-142 has been accepted by the FDA. BIIB-142 is a degrader of IRAK-4 that Biogen intends to explore for therapeutic use in patients with autoimmune diseases.
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).
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