Researchers from Guandong Pharmaceutical University reported on the synthesis and preclinical characterization of a series of novel long-acting peroxisome proliferator-activated receptor (PPAR) pan-agonists targeting PPARα, PPARδ, and PPARγ with lipid-regulating effects. PPARs are involved in lipid and lipoprotein metabolism, thus targeting the PPARs system is a promising strategy for the management of metabolic syndrome.
Researchers from Baylor University and collaborators have described the synthesis and evaluation of a series of 6-aryl-3-aroyl-indole analogues acting as tubulin polymerization inhibitors aimed to be used as anticancer agents. Inhibitors of tubulin polymerization are promising antiproliferative agents and their interaction with the colchicine site is linked to its activity as vascular disrupting agents (VDAs).
4D Molecular Therapeutics Inc. (4DMT) and Arbor Biotechnologies Inc. have established a strategic partnership focused on advancing new AAV-based gene-editing therapies for central nervous system (CNS) diseases with high unmet medical need in both rare and common disease populations.
Diabetic retinopathy is the main diabetes complication affecting the eyes, and it leads to irreversible vision loss; oxidative stress and impairment of the retinal Muller cells are among the pathogenic mechanisms. Chinese researchers presented data on adiporon, an agonist of the adiponectin receptor protein 1 (ADPOR1) and ADIPOR2 that plays a crucial role in the metabolism of lipids and glucose, in preclinical mouse models of diabetes induced by streptozotocin.
Researchers have identified a new class of antibiotics that works by blocking the transportation of lipopolysaccharide (LPS) to the outer membrane of the gram-negative bacterium Acinetobacter baumannii. The most advanced member of the class, zosurabalpin (RG-6006, Roche AG), was effective against multiple A. baumannii strains, including carbapenem-resistant and multidrug-resistant strains.
Hangzhou Yirui Pharmaceutical Technology Co. Ltd. has described N-tetrazolyl aryl urea derivatives acting as bradykinin B1 receptor antagonists reported to be useful for the treatment of age-related macular degeneration, allergic conjunctivitis, pulmonary edema, neuralgia, infectious pneumonia, diabetic retinopathy, SARS-CoV-2 infection (COVID-19) and uveitis.
Treeline Biosciences Inc. has divulged proteolysis targeting chimeras (PROTACs) compounds comprising a cereblon (CRBN) binding moiety covalently bonded to a B-cell lymphoma 6 protein (BCL6) targeting moiety through a linker reported to be useful for the treatment of cancer.
Mirati Therapeutics Inc. has identified compounds acting as GTPase KRAS and/or GTPase KRAS (mutant) inhibitors reported to be useful for the treatment of cancer.
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