Bristol Myers Squibb Co. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a DNA-binding protein Ikaros (IKZF1)-, zinc finger protein Helios (IKZF2)-, Aiolos (IKZF3)- and Eos (IKZF4)-targeting moieties through a linker.
A Vanderbilt University patent discloses new muscarinic M4 receptor positive allosteric modulators and agonists reported to be useful for the treatment of Alzheimer’s disease, pain, schizophrenia, sleep disorders and cognitive disorder.
Kymera Therapeutics Inc. has patented new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to an interleukin-1 receptor-associated kinase 1 (IRAK-4)-targeting moiety via linker.
Work at IFM Due Inc. has led to the identification of stimulator of interferon genes protein receptor (STING; TMEM173) antagonists reported to be useful for the treatment of cancer, systemic lupus erythematosus, autoinflammatory interferonopathy, rheumatoid arthritis and Aicardi-Goutieres syndrome.
Trophoblast cell surface antigen 2 (TROP2) is a transmembrane glycoprotein that acts as an intracellular calcium signal transducer, frequently overexpressed in cancer and associated with poor prognosis and disease recurrence.
Most clinically relevant T-cell receptor (TCR)-engineered T cells are typically tested in immunocompromised mice, allowing human T-cell engraftment but failing to replicate the complex interactions of a functioning immune system in patients. While humanized mouse models exist, they face challenges with incomplete immune reconstitution and technical complexity.
Researchers from University of Athens and National Centre For Scientific Research “Demokritos” have reported preclinical data from a study that aimed to assess the novel cryptochrome-2 (CRY2) stabilizer TH-301 in models of pancreatic ductal adenocarcinoma (PDAC). It was seen that treatment with TH-301 led to significant dose-, time- and cell type-dependent decreases in viability.