Organophosphorus compounds (OPs) include several types of chemical compounds used as pesticides, herbicides or nerve agents in chemical warfare that, once in the body, act by inhibiting acetylcholinesterase (AChE) functions leading to an excessive increase of acetylcholine that ultimately causes death after respiratory failure.
Norcantharidin is an active ingredient in Chinese traditional medicine that has activity against several cancer types, but its application is limited in the clinic due to toxicity and a narrow treatment window. Researchers from Tongji University and the Shanghai Institute of Materia Medica have recently described a derivative of norcantharidin – DCZ-5417 – for the potential treatment of multiple myeloma (MM).
Researchers from Multitude Therapeutics Inc. have reported the preclinical profile of AMT-253, a MUC18-targeting antibody-drug conjugate (ADC) under development for the treatment of melanoma. It comprises the anti-MUC18 humanized antibody pAb253-H linked to T1000 exatecan payload and showed superior antitumor efficacy than the traditional vc-MMAE-based ADC AMT-253-M.
Researchers at Dana-Farber Cancer Institute are advancing a fourth-generation allosteric EGFR inhibitor, EAI-432, to treat non-small-cell lung cancer driven by mutations in the EGFR gene, particularly the L858R mutation.
In stroke, one of the events underlying neuronal injury is the interaction of neuronal nitric oxide synthase (nNOS) with postsynaptic density protein 95 (PSD-95) leading to nitric oxide overproduction.
Inhibition of receptor-interacting serine/threonine-protein kinase 2 (RIPK2) has been previously described as a promising strategy for the treatment of inflammatory bowel disease, as RIPK2 is a key player in the signaling leading to bacterial peptidoglycan (PGN)-induced inflammation and it amplifies pro-inflammatory responses in the intestine.
CVI Pharmaceuticals has presented preclinical data on their thyroid hormone receptor beta (THRB) selective agonist CVI-2742 for the potential treatment of NASH. Selective activation of the THRB contributes to ameliorating the symptoms of nonalcoholic steatohepatitis (NASH), such as liver inflammation and fibrosis, hepatocyte ballooning and liver steatosis.
Researchers from Ipsen Ltd. and affiliated organizations presented the discovery and preclinical characterization of a novel NTCP inhibitor, A-7387, being developed for the treatment of HBV and HDV infections.
Nonreceptor tyrosine-protein kinase TYK2 plays key roles in the signaling of pro-inflammatory molecules such as IL-23, IL-12 or type I IFN, which at the same time play key roles in several immune-mediated diseases such as atopic dermatitis and psoriasis, among others.
It has been previously demonstrated that the two coding variants in the APOL1 gene (G1 and G2) are associated with a greater risk of progressive, proteinuric kidney disease; however, there currently are no therapies to address the causal genetic drivers of this disease. Researchers from Maze Therapeutics Inc. presented the discovery and preclinical characterization of a novel small-molecule inhibitor of APOL1, MZ-302, and they evaluated its efficacy in a new transgenic model of APOL1-mediated kidney disease (AKD).
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.webp?height=488&t=1677877909&width=650 "Epidermal growth factor receptor (EGFR)")
