Studies evaluating the in vitro and in vivo antifungal activity, hemolytic activity and cytotoxicity of COT-832, a novel polyene macrolide antifungal that is a chemical modification of amphotericin B (AmB), were presented at IDWeek by Shionogi & Co. Ltd.
EZH2 and LSD1 are histone modification enzymes often overexpressed in several types of aggressive cancer such as colorectal, breast or prostate cancer, among others.
Aberrant expression of G9a and NSD2 has been identified in multiple types of cancer. Therefore, dual-target inhibitors blocking both pathways may be considered a potential strategy to treat solid tumors. Researchers from Sun Yat-Sen University reported on the discovery and preclinical characterization of W-4032, a dual G9a/NSD2 inhibitor aimed to be used for the treatment of solid tumors.
Centessa Pharmaceuticals plc recently detailed the discovery and preclinical characterization of a novel potent and selective orexin OX2 receptor agonist, ORX-142.
B-cell lymphoma 6 (BCL6) is an essential transcriptional factor for the humoral immune response. However, genomic deregulation of BCL6 contributes to the development of different types of lymphoma such as diffuse large B-cell lymphoma (DLBCL).
To date, therapies for multiple sclerosis (MS) focus on modifying or suppressing the immune system rather than on remyelination. Recent findings have pointed to the κ-opioid receptor (KOR) as a therapeutic target for remyelination, but several KOR agonists have undesired side effects that limit their use. Researchers from the Victoria University of Wellington have tested KOR agonists derived from U-50488 in the preclinical setting for the management of MS.
Ribometrix Inc. recently discussed the discovery and preclinical evaluation of a novel potent and selective eukaryotic translation initiation factor 4E (eiF4E) inhibitor, RBX-6610, being developed for the treatment of KRAS-mutant non-small-cell lung cancer (NSCLC).
Researchers from the Chinese Academy of Medical Sciences reported the discovery of the 1,2,4-oxadiazole derivative FO-4-15 for the treatment of Alzheimer’s disease (AD).
The increasing resistance to intravenous artemisinin therapy for malaria highlights the urgent need for new treatments that offer better patient compliance and a single-dose cure to address this global health threat. Novartis AG recently presented the discovery, development and evaluation of aminoisoquinolines as fast-acting intravenous therapeutic agents for severe malaria treatment.
The University of Michigan has published details on the discovery and preclinical characterization of a new potent and selective proteolysis targeting chimera (PROTAC) degrader of BRD9, CW-3308. Synthesis and optimization of two different cereblon ligands led to the discovery of a novel series of highly potent BRD9 degraders, with CW-3308 selected as the lead candidate.
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