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Identification of Bioactive Compounds from the Roots of and Their In Silico and In Vitro AMPK Activation Potential.
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Graduate School of Pharmaceutical Sciences, College of Pharmacy, Ewha Womans University, Seoul 03760, Republic of Korea.
Libosch., which belongs to the Orobanchaceae family, is a perennial herb found in China, Japan, and Korea. In traditional medicine, it is used to cool the body, improve water metabolism in the kidney, and provide protection from metabolic diseases such as type 2 diabetes mellitus (T2DM) and obesity.
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Zhejiang Provincial Key Laboratory of Plant Evolutionary Ecology and Conservation, School of Pharmaceutical Sciences, Taizhou University, Taizhou 318000, China.
A comprehensive phytochemical investigation of the twigs/leaves and flower buds of , a rare deciduous shrub native to China, led to the isolation of 39 structurally diverse compounds. These compounds include 11 iridoid glycosides (- and -), 20 triterpenoids (, , and -), and 8 phenylpropanoids (-). Among these, amabiliosides A () and B () represent previously undescribed bis-iridoid glycosides, while amabiliosides C () and D () feature a unique bis-iridoid-monoterpenoid indole alkaloid scaffold with a tetrahydro--carboline-5-carboxylic acid moiety.
View Article and Find Full Text PDFHybrid RNA/DNA Concatemers and Self-Limited Complexes: Structure and Prospects for Therapeutic Applications.
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Institute of Chemical Biology and Fundamental Medicine SB RAS, Novosibirsk 630090, Russia.
The development of new convenient tools for the design of multicomponent nucleic acid (NA) complexes is one of the challenges in biomedicine and NA nanotechnology. In this paper, we analyzed the formation of hybrid RNA/DNA concatemers and self-limited complexes by a pair of oligonucleotides using UV melting, circular dichroism spectroscopy, and a gel shift assay. Effects of the size of the linker between duplex-forming segments of the oligonucleotides on complexes' shape and number of subunits were compared and systematized for RNA/DNA, DNA/DNA, and RNA/RNA assemblies.
View Article and Find Full Text PDFSynthesis and LDHA Inhibitory Activity of New Stiripentol-Related Compounds of Potential Use in Primary Hyperoxaluria.
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Department of Inorganic and Organic Chemistry, Faculty of Experimental Sciences, University of Jaén, Campus of International Excellence in Agri-Food (ceiA3), 23071 Jaén, Spain.
Human lactate dehydrogenase A (LDHA) is a homotetrameric isozyme involved in the conversion of glyoxylate into oxalate in the cytosol of liver cells (hepatocytes) and partially responsible for the overproduction of oxalate in patients with the rare disease called primary hyperoxaluria (PH). Recently, LDHA inhibition has been validated as a safe therapeutic method to try to control the PH disease. Stiripentol (STP) is an approved drug used in the treatment of seizures associated with Dravet's syndrome (a severe form of epilepsy in infancy) which, in addition, has been drawing interest in recent years also for potentially treating PH, due to its LDHA inhibitory activity.
View Article and Find Full Text PDFInstallation of an Indole on the BRCA1 Disordered Domain Using Triazine Chemistry.
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Department of Chemistry & Biochemistry, Texas Christian University, Fort Worth, TX 76129, USA.
The functionalization of protein sidechains with highly water-soluble chlorotriazines (or derivatives thereof) using nucleophilic aromatic substitution reactions has been commonly employed to install various functional groups, including poly(ethylene glycol) tags or fluorogenic labels. Here, a poorly soluble dichlorotriazine with an appended indole is shown to react with a construct containing the disordered domain of BRCA1. Subsequently, this construct can undergo proteolytic cleavage to remove the SUMO-tag: the -terminal poly(His) tag is still effective for purification.
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