7,314 results match your criteria possibility inhibitory


Bipartite binding of the N terminus of Skp2 to cyclin A.

Structure 2021 May 11. Epub 2021 May 11.

Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada; Department of Molecular Genetics, University of Toronto, ON M5S 1A8, Canada; Department of Biochemistry, University of Toronto, ON M5S 1A8, Canada. Electronic address:

Skp2 and cyclin A are cell-cycle regulators that control the activity of CDK2. Cyclin A acts as an activator and substrate recruitment factor of CDK2, while Skp2 mediates the ubiquitination and subsequent destruction of the CDK inhibitor protein p27. The N terminus of Skp2 can interact directly with cyclin A but is not required for p27 ubiquitination. Read More

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Ion channels and G protein-coupled receptors as targets for invertebrate pest control: from past challenges to practical insecticides.

Authors:
Yoshihisa Ozoe

Biosci Biotechnol Biochem 2021 May 14. Epub 2021 May 14.

Faculty of Life and Environmental Science, Shimane University, Matsue, Shimane 690-8504, Japan.

In the late 1970s, we discovered that toxic bicyclic phosphates inhibit the generation of miniature inhibitory junction potentials, implying their antagonism of γ-aminobutyric acid (GABA) receptors (GABARs; GABA-gated chloride channels). This unique mode of action provided a strong incentive for our research on GABARs in later years. Furthermore, minor structural changes conferred insect GABAR selectivity to this class of compounds, convincing us of the possibility of GABARs as targets for insecticides. Read More

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Physiological Characteristics and Anti-Diabetic Effect of KI62.

Food Sci Anim Resour 2021 Mar 1;41(2):274-287. Epub 2021 Mar 1.

Korea Food Research Institute, Wanju 55365, Korea.

The purpose of this study is to examine the physiological characteristics and anti-diabetic effects of KI62. The α-amylase and α-glucosidase inhibitory activity of KI62 was 94.86±3. Read More

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The Inhibitory Effect of Icariin Nanoparticles on Angiogenesis in Pulmonary Fibrosis.

J Nanosci Nanotechnol 2021 Nov;21(11):5429-5435

Linyi Traditional Chinese Medicine Hospital, Liny! 276000, Shandong, PR China.

This study investigated icariin (ICA) nanoparticles on angiogenesis in rats with pulmonary fibrosis and its mechanism. First, icariin solid nanoliposomes (ICA-SLN) were prepared. The release of icariin nanoparticles was determined using a UV-Vis spectrophotometer, after which the plasma concentration of icariin nanoparticles in rats was determined. Read More

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November 2021

Physiological concentrations of cyanide stimulate mitochondrial Complex IV and enhance cellular bioenergetics.

Proc Natl Acad Sci U S A 2021 May;118(20)

Chair of Pharmacology, Faculty of Science and Medicine, University of Fribourg, 1700 Fribourg, Switzerland

In mammalian cells, cyanide is viewed as a cytotoxic agent, which exerts its effects through inhibition of mitochondrial Complex IV (Cytochrome C oxidase [CCOx]). However, the current report demonstrates that cyanide's effect on CCOx is biphasic; low (nanomolar to low-micromolar) concentrations stimulate CCOx activity, while higher (high-micromolar) concentrations produce the "classic" inhibitory effect. Low concentrations of cyanide stimulated mitochondrial electron transport and elevated intracellular adenosine triphosphate (ATP), resulting in the stimulation of cell proliferation. Read More

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EEG coherence and power spectra during REM sleep related to melatonin intake in mild-to-moderate Alzheimer's disease: a pilot study.

Int J Neurosci 2021 May 10:1-13. Epub 2021 May 10.

Instituto Nacional de Psiquiatría "Ramón de la Fuente Muñiz", Dirección de Investigaciones en Neurociencias, Laboratorio de Cronobiología y Sueño. CDMX, México.

1. AbstractIntroduction: It has been reported that melatonin diminishes rapid eye movement (REM) sleep latency in patients with Alzheimer's disease (AD). Pharmacological studies suggest that melatonin promotes prompt sleep installation through interaction with GABA receptors, and that it is associated with acute suppression of neural electrical activity. Read More

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Chemical composition, antimicrobial, antioxidant, and cytotoxic activity of the essential oil from the leaves of Stachys pilifera Benth.

FEMS Microbiol Lett 2021 May 10. Epub 2021 May 10.

Research Laboratories in Sciences Applied to Food, Canadian Irradiation Center, INRS-Armand Frappier, Health and Biotechnology Center, Institute of Nutrition and Functional Foods, Laval, QC, Canada.

Stachys pilifera Benth is an endemic species of Stachys family found in Iran with a wide application as an herbal tea. The objective of this research was to evaluate the antimicrobial, antioxidant, and cytotoxic activity of the essential oil from the aerial parts of S. pilifera. Read More

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Anammox bacteria in treating ammonium rich wastewater: Recent perspective and appraisal.

Bioresour Technol 2021 Apr 28;334:125240. Epub 2021 Apr 28.

Ecosphere Resilience Research Centre, Faculty of Applied Sciences, University of Sri Jayewardenepura, Nugegoda, Sri Lanka. Electronic address:

The discovery of anammox process has provided eco-friendly and low-cost means of treating ammonia rich wastewater with remarkable efficiency. Furthermore, recent studies have shown that the possibility of operating the anammox process under low temperatures and high organic matter contents broadening the application of the anammox process. However, short doubling time and extensive levels of sensitivity towards nutrients and environmental alterations such as salinity and temperature are the limitations in practical applications of the anammox process. Read More

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Engineered microRNA-based regulatory element permits safe high-dose miniMECP2 gene therapy in Rett mice.

Brain 2021 May 5. Epub 2021 May 5.

Department of Pediatrics, University of Texas Southwestern Medical Center, Dallas, TX, 75390, USA.

MECP2 gene transfer has been shown to extend the survival of Mecp2-/y knockout (KO) mice modeling Rett syndrome (RTT), an X-linked neurodevelopmental disorder. However, controlling deleterious overexpression of MeCP2 remains the critical unmet obstacle towards a safe and effective gene therapy approach for RTT. A recently developed truncated miniMECP2 gene has also been shown to be therapeutic after AAV9-mediated gene transfer in KO neonates. Read More

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Amphetamine-Decreased Progesterone and Estradiol Release in Rat Granulosa Cells: The Regulatory Role of cAMP- and Ca-Mediated Signaling Pathways.

Biomedicines 2021 Apr 29;9(5). Epub 2021 Apr 29.

Institute of Sports Sciences, University of Taipei, Taipei City 112, Taiwan.

The purpose of this study is to evaluate the amphetamine effects on progesterone and estradiol production in rat granulosa cells and the underlying cellular regulatory mechanisms. Freshly dispersed rat granulosa cells were cultured with various test drugs in the presence of amphetamine, and the estradiol/progesterone production and the cytosolic cAMP level were measured. Additionally, the cytosolic-free Ca concentrations ([Ca]i) were measured to examine the role of Ca influx in the presence of amphetamine. Read More

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Investigation of an ALDH1A1-specific inhibitor for suppression of weight gain in a diet-induced mouse model of obesity.

Int J Obes (Lond) 2021 May 1. Epub 2021 May 1.

Department of Comparative Medicine, University of Washington, Seattle, WA, USA.

Background: Retinoic acid (RA) controls diverse physiological functions including weight regulation and energy metabolism. It has been reported that mice lacking ALDH1A1, one of the aldehyde dehydrogenases (ALDH) that synthesize RA, are healthy and resistant to weight gain, raising the possibility that inhibiting this enzyme might treat obesity. We previously demonstrated that treatment with a pan-ALDH1A enzyme inhibitor, WIN18446, suppressed weight gain in mice fed a high-fat diet (HFD), but caused increased hepatic lipidosis and reversible male infertility. Read More

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Microglia Specific Drug Targeting Using Natural Products for the Regulation of Redox Imbalance in Neurodegeneration.

Front Pharmacol 2021 13;12:654489. Epub 2021 Apr 13.

Biochemistry and Molecular Biology Laboratory, Department of Zoology, Banaras Hindu University, Varanasi, India.

Microglia, a type of innate immune cell of the brain, regulates neurogenesis, immunological surveillance, redox imbalance, cognitive and behavioral changes under normal and pathological conditions like Alzheimer's, Parkinson's, Multiple sclerosis and traumatic brain injury. Microglia produces a wide variety of cytokines to maintain homeostasis. It also participates in synaptic pruning and regulation of neurons overproduction by phagocytosis of neural precursor cells. Read More

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Identification of Novel Inhibitors of DNA Ligase (LigA).

Molecules 2021 Apr 25;26(9). Epub 2021 Apr 25.

School of Biological Sciences and Institute of Biological and Biomedical Sciences, University of Portsmouth, Portsmouth PO1 2DY, UK.

Present in all organisms, DNA ligases catalyse the formation of a phosphodiester bond between a 3' hydroxyl and a 5' phosphate, a reaction that is essential for maintaining genome integrity during replication and repair. Eubacterial DNA ligases use NAD as a cofactor and possess low sequence and structural homology relative to eukaryotic DNA ligases which use ATP as a cofactor. These key differences enable specific targeting of bacterial DNA ligases as an antibacterial strategy. Read More

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Tight Junction Protein Claudin-12 Is Involved in Cell Migration during Metastasis.

Biomolecules 2021 Apr 25;11(5). Epub 2021 Apr 25.

Department of Developmental Biology, Plovdiv University "Paisii Hilendarski", 4000 Plovdiv, Bulgaria.

Claudins are important components of the tight junctions determining barrier properties, cell polarity, and paracellular permeability. Although many functions of claudins in cancer cells have not been elucidated, recent studies have shown that claudins play an important role in cell migration and metastasis. Loss of epithelial/endothelial integrity, disruption of tight junctions, and increased paracellular leakage are often observed during metastasis. Read More

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A Review on Health-Promoting, Biological, and Functional Aspects of Bioactive Peptides in Food Applications.

Biomolecules 2021 Apr 23;11(5). Epub 2021 Apr 23.

Centro Tecnológico de la Carne de Galicia, Rúa Galicia No. 4, Parque Tecnológico de Galicia, San Cibrao das Viñas, 32900 Ourense, Spain.

Food-derived bioactive peptides are being used as important functional ingredients for health-promoting foods and nutraceuticals in recent times in order to prevent and manage several diseases thanks to their biological activities. Bioactive peptides are specific protein fractions, which show broad applications in cosmetics, food additives, nutraceuticals, and pharmaceuticals as antimicrobial, antioxidant, antithrombotic, and angiotensin-I-converting enzyme (ACE)-inhibitory ingredients. These peptides can preserve consumer health by retarding chronic diseases owing to modulation or improvement of the physiological functions of human body. Read More

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Triphenilphosphonium Analogs of Chloramphenicol as Dual-Acting Antimicrobial and Antiproliferating Agents.

Antibiotics (Basel) 2021 Apr 23;10(5). Epub 2021 Apr 23.

Department of Chemistry, Lomonosov Moscow State University, Leninskie Gory 1, 119991 Moscow, Russia.

In the current work, in continuation of our recent research, we synthesized and studied new chimeric compounds, including the ribosome-targeting antibiotic chloramphenicol (CHL) and the membrane-penetrating cation triphenylphosphonium (TPP), which are linked by alkyl groups of different lengths. Using various biochemical assays, we showed that these CAM-Cn-TPP compounds bind to the bacterial ribosome, inhibit protein synthesis in vitro and in vivo in a way similar to that of the parent CHL, and significantly reduce membrane potential. Similar to CAM-C4-TPP, the mode of action of CAM-C10-TPP and CAM-C14-TPP in bacterial ribosomes differs from that of CHL. Read More

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Antibacterial and Antifungal Studies of Biosynthesized Silver Nanoparticles against Plant Parasitic Nematode Plant Pathogens and .

Molecules 2021 Apr 23;26(9). Epub 2021 Apr 23.

CONACYT Research Fellow at Centro de Nanociencias y Nanotecnología, Universidad Nacional Autónoma de México, 22800 Ensenada, Baja California, Mexico.

The possibility of using silver nanoparticles (AgNPs) to enhance the plants growth, crop production, and control of plant diseases is currently being researched. One of the most effective approaches for the production of AgNPs is green synthesis. Herein, we report a green and phytogenic synthesis of AgNPs by using aqueous extract of strawberry waste (solid waste after fruit juice extraction) as a novel bioresource, which is a non-hazardous and inexpensive that can act as a reducing, capping, and stabilizing agent. Read More

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Dual Role for Astroglial Copper-Assisted Polyamine Metabolism during Intense Network Activity.

Biomolecules 2021 Apr 19;11(4). Epub 2021 Apr 19.

Functional Pharmacology Research Group, Research Centre for Natural Sciences, Institute of Organic Chemistry, H-1117 Budapest, Hungary.

Astrocytes serve essential roles in human brain function and diseases. Growing evidence indicates that astrocytes are central players of the feedback modulation of excitatory Glu signalling during epileptiform activity via Glu-GABA exchange. The underlying mechanism results in the increase of tonic inhibition by reverse operation of the astroglial GABA transporter, induced by Glu-Na symport. Read More

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Null Effect of Transcranial Static Magnetic Field Stimulation over the Dorsolateral Prefrontal Cortex on Behavioral Performance in a Go/NoGo Task.

Brain Sci 2021 Apr 11;11(4). Epub 2021 Apr 11.

Department of Sensorimotor Neuroscience, Graduate School of Biomedical and Health Sciences, Hiroshima University, Hiroshima 734-8553, Japan.

The purpose of this pilot study was to investigate whether transcranial static magnetic field stimulation (tSMS), which can modulate cortical excitability, would influence inhibitory control function when applied over the dorsolateral prefrontal cortex (DLPFC). Young healthy adults ( = 8, mean age ± SD = 24.4 ± 4. Read More

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Synthesis, Biological Activity, and Molecular Dynamics Study of Novel Series of a Trimethoprim Analogs as Multi-Targeted Compounds: Dihydrofolate Reductase (DHFR) Inhibitors and DNA-Binding Agents.

Int J Mol Sci 2021 Apr 1;22(7). Epub 2021 Apr 1.

Department of Organic Chemistry, Medical University of Bialystok, 15-222 Bialystok, Poland.

Eighteen previously undescribed trimethoprim (TMP) analogs containing amide bonds () were synthesized and compared with TMP, methotrexate (MTX), and netropsin (NT). These compounds were designed as potential minor groove binding agents (MGBAs) and inhibitors of human dihydrofolate reductase (DHFR). The all-new derivatives were obtained via solid phase synthesis using 4-nitrophenyl Wang resin. Read More

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Basal ganglia and cortical control of thalamic rebound spikes.

Eur J Neurosci 2021 Apr 29. Epub 2021 Apr 29.

Department of Psychology, University of Sheffield, Sheffield, UK.

Movement-related decreases in firing rate have been observed in basal ganglia output neurons. They may transmit motor signals to the thalamus, but the effect of these firing rate decreases on downstream neurons in the motor thalamus is not known. One possibility is that they lead to thalamic post-inhibitory rebound spikes. Read More

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Personalized cognitive training: Protocol for individual-level meta-analysis implementing machine learning methods.

J Psychiatr Res 2021 Mar 31;138:342-348. Epub 2021 Mar 31.

Department of Psychology, School of Psychological Sciences, University of Haifa, Haifa, Israel; The Integrated Brain and Behavior Research Center (IBBR), University of Haifa, Haifa, Israel.

Accumulating evidence suggests that cognitive training may enhance well-being. Yet, mixed findings imply that individual differences and training characteristics may interact to moderate training efficacy. To investigate this possibility, the current paper describes a protocol for a data-driven individual-level meta-analysis study aimed at developing personalized cognitive training. Read More

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Real-Time Respiration Changes as a Viability Indicator for Rapid Antibiotic Susceptibility Testing in a Microfluidic Chamber Array.

ACS Sens 2021 Apr 26. Epub 2021 Apr 26.

Department of Biosystems Science and Engineering, Bioanalytics Group, ETH Zürich, Mattenstrasse 26, 4058 Basel, Switzerland.

Rapid identification of a pathogen and the measurement of its antibiotic susceptibility are key elements in the diagnostic process of bacterial infections. Microfluidic technologies offer great control over handling and manipulation of low sample volumes with the possibility to study microbial cultures on the single-cell level. Downscaling the dimensions of cultivation systems directly results in a lower number of bacteria required for antibiotic susceptibility testing (AST) and thus in a reduction of the time to result. Read More

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A pain killer without analgesic tolerance designed by co-targeting PSD-95-nNOS interaction and α2-containning GABARs.

Theranostics 2021 3;11(12):5970-5985. Epub 2021 Apr 3.

Department of Pharmacology, School of Pharmacy, Nanjing Medical University, China.

Overactivation of N-methyl-D-aspartate receptor (NMDAR) in the spinal cord dorsal horn (SDH) in the setting of injury represents a key mechanism of neuropathic pain. However, directly blocking NMDAR or its downstream signaling, interaction between postsynaptic density-95 (PSD-95) and neuronal nitric oxide synthase (nNOS), causes analgesic tolerance, mainly due to GABAergic disinhibition. The aim of this study is to explore the possibility of preventing analgesic tolerance through co-targeting NMDAR downstream signaling and γ-aminobutyric acid type A receptors (GABARs). Read More

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The Calcium-Activated Chloride Channel TMEM16A is Inhibitied by Liquiritigenin.

Front Pharmacol 2021 8;12:628968. Epub 2021 Apr 8.

Department of Physiology, Showa University School of Medicine, Tokyo, Japan.

The transmembrane 16 (TMEM16) family contains 10 subtypes, and the function of each protein is different. TMEM16A is a calcium-activated chloride channel involved in physiological and pathological situations. Liquiritigenin is an aglycone derived from , and it is generated via the metabolism of enterobacterial flora. Read More

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Unraveling the mechanisms of surround suppression in early visual processing.

PLoS Comput Biol 2021 Apr 22;17(4):e1008916. Epub 2021 Apr 22.

Courant Institute of Mathematical Sciences, New York University, New York, New York, United States of America.

This paper uses mathematical modeling to study the mechanisms of surround suppression in the primate visual cortex. We present a large-scale neural circuit model consisting of three interconnected components: LGN and two input layers (Layer 4Ca and Layer 6) of the primary visual cortex V1, covering several hundred hypercolumns. Anatomical structures are incorporated and physiological parameters from realistic modeling work are used. Read More

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A target safety assessment of the potential toxicological risks of targeting plasmepsin IX/X for the treatment of malaria.

Toxicol Res (Camb) 2021 Mar 15;10(2):203-213. Epub 2021 Feb 15.

ApconiX, Alderley Park, Alderley Edge, SK10 4TG, UK.

The aspartic proteases plasmepsin IX/X are important antimalarial drug targets due to their specificity to the malaria parasite and their vital role as mediators of disease progression. Focusing on parasite-specific targets where no human homologue exists reduces the possibility of on-target drug toxicity. However, there is a risk of toxicity driven by inadequate selectivity for plasmepsins IX/X in Plasmodium over related mammalian aspartic proteases. Read More

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Anti-Microbial Potential of Nano-Emulsion form of Essential Oil Obtained from Aerial Parts of L. as Food Additive.

Adv Pharm Bull 2021 Feb 23;11(2):327-334. Epub 2020 Feb 23.

Department of Pharmacognosy and Biotechnology, Pharmaceutical Sciences Research Center, Hemoglobinopathy Institute, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

Foodborne diseases are still a serious problem in public health and natural compounds are being widely considered for their potential industrial protective additive in food products. L. has been known as an antimicrobial effective herb. Read More

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February 2021

Natural polyketide 6-pentyl-2-pyrone-2-one and its synthetic analogues efficiently prevent marine biofouling.

Biofouling 2021 Apr 18:1-10. Epub 2021 Apr 18.

Department of Marine Biotechnology, National Sun Yat-sen University, Kaohsiung, Taiwan, ROC.

Biofouling is a widespread phenomenon in oceans worldwide. With increasing human development and activities in open and coastal waters, and due to the environmental impact of AF organotins and copper-based paint, the demand for nontoxic antifouling (AF) paints is increasing. Various bioassays for antimicrobial activity, anti-biofilm formation and anti-barnacle settlement were established to evaluate the possibility of using marine natural products as AF agents. Read More

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