Researchers at Lawrence Livermore National Laboratory, Leidos Biomedical Research Inc. and Theras Inc. (dba Bridgebio Oncology Therapeutics) have described GTPase KRAS (G12C mutant) inhibitors reported to be useful for the treatment of cancer.
Daiichi Sankyo Co. Ltd. has divulged compounds acting as NLRP3 inflammasome inhibitors reported to be useful for the treatment of inflammation, major depression, multiple sclerosis, multiple system atrophy, schizophrenia, autoimmune disease, Alzheimer’s disease and Parkinson’s disease, among others.
Disarm Therapeutics Inc. has identified NAD(+) hydrolase SARM1 (SAMD2; MyD88-5) inhibitors reported to be useful for the treatment of amyotrophic lateral sclerosis, multiple sclerosis, diabetic neuropathy and chemotherapy-induced peripheral neuropathy.
Mwyngil Therapeutics Inc. has synthesized compounds acting as NLRP3 inflammasome inhibitors reported to be useful for the treatment of arthritis, nonalcoholic or metabolic dysfunction-associated steatohepatitis (NASH/MASH), osteoporosis, hypertension, inflammation, SARS-CoV-2 infection (COVID-19), autoimmune disease and Alzheimer’s disease, among others.
In mammals, the disruptor of telomeric silencing 1-like (DOT1L) is the only methyltransferase that catalyzes the mono-, di- and tri-methylation of histone H3 at lysine 79 (H3K79). The DOT1L/H3K79me is involved in several relevant physiological and pathological mechanisms, including several viral infections.
Azitra Inc. has obtained IND clearance from the FDA for a first-in-human phase I/II study of ATR-04 for moderate to severe EGFR inhibitor-associated dermal toxicity. The study is expected to begin by year-end.
IGC Pharma Inc. has reported preclinical research demonstrating the therapeutic potential of IGC-1C, a cyclic dipeptide-based small-molecule modulator, in neurodegenerative disease due to its modulation of tau protein, which is involved in the formation of neurofibrillary tangles, a key hallmark of Alzheimer’s disease.
Simcere Zaiming Pharmaceutical Co. Ltd. has obtained clinical trial approval from China’s National Medical Products Administration (NMPA) for SIM-0508, a small-molecule inhibitor of DNA polymerase θ (POLθ), allowing initiation of clinical trials in locally advanced or metastatic solid tumors.
At the recently concluded ACS Fall meeting, Bristol Myers Squibb Co. reported the discovery of potent orally bioavailable B-cell lymphoma 6 protein (BCL6) ligand-directed degraders (LDDs).
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