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Identifying the wide diversity of extraterrestrial purine and pyrimidine nucleobases in carbonaceous meteorites
The lack of pyrimidine diversity in meteorites remains a mystery since prebiotic chemical models and laboratory experiments have predicted that these...
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Electrochemical behavior and theoretical studies of arylazo (1-naphthyl-2-cyanoacetamide) derivatives as new corrosion inhibitors for Inconel 800 in chloride solution
In this study, synthesize and insight the corrosion inhibition properties of two novel derivatives of 1-naphthyl-2-cyanoacetamide (NCDs)...
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Small-molecule inhibition of Lats kinases may promote Yap-dependent proliferation in postmitotic mammalian tissues
Hippo signaling is an evolutionarily conserved pathway that restricts growth and regeneration predominantly by suppressing the activity of the...
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On the function of biosynthesized cellulose as barrier against bacterial colonization of VAD drivelines
Bacterial colonization of drivelines represents a major adverse event in the implantation of left ventricular assist devices (L-VADs) for the...
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Peptidomimetics designed to bind to RAS effector domain are promising cancer therapeutic compounds
Oncogenic RAS proteins are important for driving tumour formation, and for maintenance of the transformed phenotype, and thus their relevance as a...
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Rab4A-directed endosome traffic shapes pro-inflammatory mitochondrial metabolism in T cells via mitophagy, CD98 expression, and kynurenine-sensitive mTOR activation
Activation of the mechanistic target of rapamycin (mTOR) is a key metabolic checkpoint of pro-inflammatory T-cell development that contributes to the...
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Inhibition of mitochondrial folate metabolism drives differentiation through mTORC1 mediated purine sensing
Supporting cell proliferation through nucleotide biosynthesis is an essential requirement for cancer cells. Hence, inhibition of folate-mediated one...
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Green Synthesis of Substituted Anilines and Quinazolines from Isatoic Anhydride-8-amide
Synthetic methods used to generate substituted anilines and quinazolines, both privileged pharmacological structures, are cumbersome, hazardous or,...
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Compounds targeting OSBPL7 increase ABCA1-dependent cholesterol efflux preserving kidney function in two models of kidney disease
Impaired cellular cholesterol efflux is a key factor in the progression of renal, cardiovascular, and autoimmune diseases. Here we describe a class...
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Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation
Narcolepsy type 1 (NT1) is a chronic neurological disorder that impairs the brain’s ability to control sleep-wake cycles. Current therapies are...
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A new antiviral scaffold for human norovirus identified with computer-aided approaches on the viral polymerase
Human norovirus is the leading cause of acute gastroenteritis worldwide, affecting every year 685 million people. In about one third of cases, this...
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The first Q-Tube based high-pressure synthesis of anti-cancer active thiazolo[4,5-c]pyridazines via the [4 + 2] cyclocondensation of 3-oxo-2-arylhydrazonopropanals with 4-thiazolidinones
A novel and efficient protocol for the synthesis of thiazolo[4,5- c ]pyridazine derivatives was developed. The approach utilizes a high pressure Q-Tube...
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A Cell-based Screen in Actinomyces oris to Identify Sortase Inhibitors
Sortase enzymes are attractive antivirulence drug targets that attach virulence factors to the surface of Staphylococcus aureus and other medically...
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β-carboline biomediators induce reveromycin production in Streptomyces sp. SN-593
The biosynthetic potential of soil-dwelling actinomycetes to produce diverse bioactive molecules that are useful as drug seeds has been achieved in...
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Modified aptamers as reagents to characterize recombinant human erythropoietin products
Reliable and reproducible monitoring of the conformational state of therapeutic protein products remains an unmet technological need. This need is...
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RETRACTED ARTICLE: Dietary metabotype modelling predicts individual responses to dietary interventions
Habitual consumption of poor quality diets is linked directly to risk factors for many non-communicable diseases. This has resulted in the vast...
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Site-specific allylic C–H bond functionalization with a copper-bound N-centred radical
Methods for selective C–H bond functionalization have provided chemists with versatile and powerful toolboxes for synthesis, such as the late-stage...
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Dual-active antifungal agents containing strobilurin and SDHI-based pharmacophores
Crop disease management often implies repeated application of fungicides. However, the increasing emergence of fungicide-resistant pathogens requires...
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The compound TB47 is highly bactericidal against Mycobacterium ulcerans in a Buruli ulcer mouse model
Buruli ulcer (BU) is an emerging infectious disease that causes disfiguring skin ulcers. The causative agent, Mycobacterium ulcerans , secretes toxin...
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SLC25A51 is a mammalian mitochondrial NAD+ transporter
Mitochondria require nicotinamide adenine dinucleotide (NAD + ) to carry out the fundamental processes that fuel respiration and mediate cellular...