Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has disclosed proteolysis targeting chimeric (PROTAC) compounds comprising cereblon (CRBN) ligands covalently bonded to a B-cell lymphoma 6 protein (BCL6)-targeting moiety through a linker.
IKZF2, a transcription factor in the Ikaros family, plays a key role in stabilizing regulatory T (Treg) cells and promoting immune suppression within the tumor microenvironment (TME). Selective targeting of IKZF2 in intratumoral Tregs has the potential to enhance antitumor immunity and improve the efficacy of immunotherapy, while minimizing immune-related toxicities associated with systemic Treg depletion.
Beactica Therapeutics AB has held a first scientific advisory meeting with the Swedish Medical Products Agency (MPA) for BEA-17, the company’s first-in-class small-molecule targeted degrader of lysine demethylase 1 (LSD1) and its co-factor CoREST.
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.
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