Fractalkine, when binding to its receptor CX3CR1, modulates leukocyte adhesion and acts as a chemotactic agent. The expression of cardiac CX3CR1/fractalkine is elevated in patients with heart failure and CX3CR1 antagonists may improve the cardiac function by modulation of this axis.
Pfizer Inc. provided details on the discovery and in vitro/in vivo characteristics of SIK inhibitor PF-07899895 for the treatment of inflammatory bowel disease (IBD). Pfizer’s program focused on pan-SIK inhibition to regulate cytokine production in immune cells based on the hypothesis that this approach could suppress pro-inflammatory cytokines/chemokines and promote an anti-inflammatory phenotype.
It is known that phosphatidylinositol 5-phosphate 4-kinase, type II, γ (PIP4K2C) is a lipid kinase tied to poor outcomes in a variety of cancers, such as colorectal (CRC) and breast cancers. In the search for PIP4K2C degraders, researchers from Larkspur Biosciences Inc. discovered LRK-4189, a cereblon-mediated PIP4K2C degrader.
At the 12th Aging Research & Drug Discovery (ARDD) Meeting, which is being held this week in Copenhagen, Life Biosciences Inc. announced that it is developing its partial epigenetic reprogramming technology for liver disease as well as optic neuropathies. The company’s chief scientific officer Sharon Rosenzweig-Lipson estimated that its ER-100 would enter clinical trials in early 2026, putting it on track to be the first application of partial epigenetic reprogramming to enter the clinic.
At last week’s American Chemical Society meeting, Novartis AG presented the discovery of IID-432, a highly efficacious and safe inhibitor of Trypanosoma cruzi topoisomerase 2 (Top2), offering a short-duration curative treatment for Chagas disease.
Researchers from Arkansas State University synthesized a library of thiazole derivatives, and these compounds were subsequently screened for their antibacterial activity both in vitro and in vivo.
Genfleet Therapeutics Co. Ltd. has presented preclinical data on their KRAS G12C inhibitor fulzerasib, also known as GFH-925, the third approved KRAS G12C inhibitor for treating non-small-cell lung cancer (NSCLC).
RAS is the most mutated oncogene in cancer (about 30% rate), where mutations in KRAS are the most prevalent. The approval of covalent KRAS G12C inhibitors has shown allosteric inhibition of KRAS to be a feasible therapeutic strategy, and there is interest in developing new KRAS-directed therapies to target additional KRAS mutants. Amgen has presented data regarding its pan-KRAS inhibitor AMG-410.
Microglia are the brain’s innate immune cells that maintain brain health and play a key role in Alzheimer's disease (AD). Triggering receptor expressed on myeloid cells 2 (TREM2) acts as a regulator of microglial cells and restores neuronal functioning.
Researchers from Ovid Therapeutics Inc. presented preclinical efficacy data on the combination of OV-329, a small-molecule inhibitor of the mitochondrial GABA aminotransferase (GABA-AT) enzyme, with docetaxel in a murine intracardiac model of triple-negative breast cancer (TNBC).
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