Methionine adenosyltransferase 2A (MAT2A), the rate-limiting enzyme in the methionine cycle, catalyzes the formation of S-adenosylmethionine (SAM) from methionine and adenosine triphosphate (ATP).
Malaria is caused by Plasmodium species that infect hundreds of millions of people annually. Among the plasmodia, Plasmodium falciparum is considered the most dangerous due to frequent severe clinical complications and high mortality rates. Researchers from the University of California at Riverside described the discovery and mechanism of action of MED-6189, a kalihinol analog effective against drug-sensitive and drug-resistant P. falciparum strains in vitro and in vivo.
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).
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