The elaboration of previously reported indole fragments as inhibitors of inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis, in vitro inhibitory values for IMPDH II, PBMC proliferation and physicochemical properties are discussed.
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http://dx.doi.org/10.1016/j.bmcl.2006.01.090 | DOI Listing |
Cell Mol Biol (Noisy-le-grand)
January 2025
College of Life Sciences, Liaoning Normal University, Dalian 116000, Liaoning Province, China.
Liaoning cashmere goat is an outstanding breed in China primarily for cashmere production, with strict controls against genetic outflow. Melatonin(MT) is a key factor affecting cashmere growth, and preliminary transcriptome sequencing indicated that melatonin upregulates the expression of the PIP5K1A gene in skin fibroblasts. To predict the physicochemical properties of PIP5K1A in Liaoning cashmere goats, ascertain the tissue localization of PIP5K1A in their skin, and explore the role and mechanism of PIP5K1A in the proliferation of skin fibroblasts.
View Article and Find Full Text PDFNPJ Vaccines
January 2025
Department of Microbial Infection and Immunity, College of Medicine, The Ohio State University, Columbus, OH, USA.
Natural killer (NK) cell-driven effector mechanisms, such as antibody-dependent cell-mediated cytotoxicity, emerged as a secondary correlate of protection in the RV144 HIV vaccine clinical trial, the only vaccine thus far demonstrating some efficacy in human trials. Therefore, leveraging NK cells with enhanced cytotoxic effector responses may bolster vaccine-induced protection against HIV. Here, we investigated the effect of orally administering indole-3-carbinol (I3C), an aryl hydrocarbon receptor (AHR) agonist, as an adjuvant to an RV144-like vaccine platform in a mouse model.
View Article and Find Full Text PDFPest Manag Sci
January 2025
State Key Laboratory for Biology of Plant Diseases and Insect Pests, Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing, China.
Background: Bactrocera cucurbitae (Coquillett) is a distructive quarantine insect pest that causes significant economic losses on cucurbit crops. To explore a green control approach, we investigated the behavioral responses of B. cucurbitae larvae and adults to bacterial suspensions, sediments, and supernatants derived from eight gut microbial strains across four distinct genera.
View Article and Find Full Text PDFMolecules
December 2024
Ufa Institute of Chemistry, Ufa Federal Research Centre, Russian Academy of Science, 71, Prospect Octyabrya, Ufa 450054, Russia.
Alzheimer's disease (AD) poses a significant public health issue. Despite the fact that today there are several methods of maintenance therapy, one of the most widely used methods is designed to correct the deficiency of acetylcholine. In the search for new potential inhibitors of cholinesterase enzymes, eight new derivatives of 3-oxo- or 2,3-indolo-triterpenic acid conjugated with amino-quinuclidine bicyclic cores were designed and synthesized.
View Article and Find Full Text PDFMolecules
December 2024
Institut für Pharmazeutische und Medizinische Chemie, Universität Münster, Corrensstraße 48, D-48149 Münster, Germany.
The serine/threonine kinase CK2 (formerly known as casein kinase II) plays a crucial role in various CNS disorders and is highly expressed in various types of cancer. Therefore, inhibiting this key kinase could be promising for the treatment of these diseases. The CK2 holoenzyme is formed by the recruitment of two catalytically active CK2α and/or CK2α' subunits by a regulatory CK2β dimer.
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