Beijing DP Technology Co. Ltd. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently bonded to a Myc proto-oncogene protein (c-Myc)-targeting moiety through a linker reported to be useful for the treatment of cancer, viral infections, and cardiovascular, immunological and cerebrovascular disorders.
Interleukin-1 receptor-associated kinase 4 (IRAK-4) is a modulator of IL-1 receptor and Toll-like receptor (TLR) signaling and has emerged as a promising therapeutic target for several inflammatory diseases. Gilead Sciences Inc. and Nurix Therapeutics Inc. recently presented data generated in a preclinical murine model of AD with their IRAK-4 degrader GS-6791.
Amphista Therapeutics Ltd. has disclosed first data on its TEAD oncology therapeutic program. The company’s TEAD Targeted Glues are inherently smaller and more drug-like molecules than conventional PROTAC binders.
China Pharmaceutical University has patented non-ubiquitin proteolysis targeting chimera (NuTACs) comprising proteasomal ubiquitin receptor ADRM1 (ARM1; hRpn13) linked to programmed cell death 1 ligand 1 (CD274; PD-L1) and/or bromodomain-containing protein 4 (BRD4; HUNK1)-targeting moiety. They are reported to be useful for the treatment of cancer, eye disorders, viral infections, autoimmune diseases, inflammatory disorders and systemic inflammatory response syndrome.
Monte Rosa Therapeutics Inc. has synthesized molecular glue degraders comprising a E3 ubiquitin-protein ligase binding moiety coupled to a cyclin-dependent kinase 2 (CDK2)-targeting moiety acting as cyclin-dependent kinase 2 (CDK2) degradation inducers potentially useful for the treatment of cancer.
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.
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