Researchers from Arkuda Therapeutics reported the discovery and preclinical evaluation of novel oxazoline enhancers of cellular progranulin (PGRN) secretion as candidates for cognition disorders therapy. Phenotypic screening of a diverse library of compounds was applied with the aim of identifying structures that effectively enhanced PGRN release. The lead hits were optimized and assessed in an immortalized murine microglial cell line (BV-2).
Using a near-atomic resolution cryo-electron microscope and imaging techniques that prevent loss of information, scientists at the La Jolla Institute for Immunology (LJI) and Regeneron Pharmaceuticals Inc. have obtained the complete 3D structure of the glycoprotein of the Ebola virus and that of the drug that neutralizes it, Inmazeb, the first FDA-approved treatment for this deadly virus. “The challenge was embracing the inherent asymmetry, the heterogeneity that is really there in biology, understanding it and collecting enough data to get all the images without needing to force any symmetry averaging,” senior author Erica Ollmann Saphire told BioWorld.
Wigen Biomedicine Technology (Shanghai) Co. Ltd. has described 1,2,4-triazolone derivatives acting as dihydroorotate dehydrogenase (DHODH) inhibitors reported to be useful for the treatment of solid tumors and hematologic blood cancer.
Humanwell Healthcare (Group) Co. Ltd. has identified transcriptional enhancer factor (TEAD) inhibitors reported to be useful for the treatment of cancer.
Shanghai Aryl Pharmtech Co. Ltd. and Zhejiang Hisun Pharmaceutical Co. Ltd. have divulged trideuteromethyl-substituted pyrazino pyrazino quinolinone derivatives acting as deuterated GTPase KRAS (mutant) inhibitors reported to be useful for the treatment of cancer.
Biogen Inc. and C4 Therapeutics Inc. have synthesized proteolysis targeting chimeric (PROTAC) compounds comprising cereblon (CRBN) ligands covalently linked to an IL-1 receptor-associated kinase 4 (IRAK-4)-targeting moiety through a linker.
Sichuan Kelun-Biotech Biopharmaceutical Co. Ltd. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a GTPase KRAS (G12D mutant) targeting moiety reported to be useful for the treatment of cancer.
Accutar Biotechnology Inc. has received FDA clearance of its IND application for AC-0676 for the treatment of patients with relapsed/refractory B-cell malignancies.
Lung and pancreatic cancer cells usually become chemotherapy resistant; the alternative to target nonapoptotic pathways was hypothesized as an approach for treating these cancers. Researchers from Sun Yat-sen University and their collaborators focused on the activation of pyroptosis as a therapeutic alternative to treat these resistant tumor types.
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