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PubMed Journals Articles About "Discovery Betulinaldehyde Natural Agonist" RSS

16:26 EDT 16th July 2019 | BioPortfolio

Discovery Betulinaldehyde Natural Agonist PubMed articles on BioPortfolio. Our PubMed references draw on over 21 million records from the medical literature. Here you can see the latest Discovery Betulinaldehyde Natural Agonist articles that have been published worldwide.

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Showing "Discovery betulinaldehyde natural agonist" PubMed Articles 1–25 of 8,700+

Novel Methylated DNA Markers Discriminate Advanced Neoplasia in Pancreatic Cysts: Marker Discovery, Tissue Validation, and Cyst Fluid Testing.

Pancreatic cystic lesions (PCLs) may be precancerous. Those likely to harbor high-grade dysplasia (HGD) or pancreatic cancer (PC) are targets for surgical resection. Current algorithms to predict advanced neoplasia (HGD/PC) in PCLs lack diagnostic accuracy. In pancreatic tissue and cyst fluid (CF) from PCLs, we sought to identify and validate novel methylated DNA markers (MDMs) that discriminate HGD/PC from low-grade dysplasia (LGD) or no dysplasia (ND).


Andrographolide sensitizes Hep-2 human laryngeal cancer cells to carboplatin-induced apoptosis by increasing reactive oxygen species levels.

Andrographolide is a natural diterpenoid from Andrographis paniculata that has been proposed as an anticancer agent as well as a chemosensitizer for use in combination with anticancer drugs. Carboplatin is the first-line chemotherapeutic agent for advanced laryngeal carcinoma. However, the clinical efficacy of carboplatin is limited by drug resistance and side effects. The aim of this study was to investigate whether andrographolide has a synergistic antitumor effect with carboplatin on human laryngeal canc...

Approach to tapering antisarcoidosis therapy.

Sarcoidosis is a multisystemic granulomatous disease, which commonly affects the lung. The natural course of the disease and prognosis are variable from asymptomatic, spontaneous remission to progressive disease, which requires treatment. Once treatment is initiated, tapering therapy can be problematic.


Suboptimal stimulation by weak agonist epitope variants does not drive dysfunction of HIV-1-specific cytotoxic T lymphocyte clones.

To assess whether weakly recognized epitope variants induce anergy in HIV-1-specific CD8 T lymphocyte (CTL) clones as a mechanism of dysfunction.

Autoantibodies in chronic inflammatory demyelinating polyradiculoneuropathy.

Chronic inflammatory demyelinating polyradiculoneuropathy (CIDP) is a heterogeneous disorder that includes diverse clinical presentations and immunopathological mechanisms. Antibodies targeting proteins of the node of Ranvier are present in a subset of CIDP patients. These autoantibodies are pathogenic and associate with specific clinical phenotypes and therapeutic peculiarities. This review summarizes the novel insights that the discovery of novel autoantibodies has brought to the understanding of CIDP.

The Successful Sequential Use of Plerixafor and Eltrombopag For Hematopoietic Cell Transplantation in a Child With High-Risk Neuroblastoma.

High-dose chemotherapy with autologous hematopoietic stem cell transplantation improves event-free survival in patients with high-risk neuroblastoma. However, in heavily pretreated patients, poor marrow function can be an obstacle in the successful proceeding of therapy. Priming with plerixafor plus filgrastim is an option for effective mobilization and collection of stem cells. In addition, thrombopoietin agonist eltrombopag can improve the outcome of posttransplantation thrombocytopenia and poor graft fun...

The pharmacodynamic effects of a dopamine-somatostatin chimera agonist on the cardiovascular system.

The quantification of the effect of pharmacological treatment on the cardiovascular system is complicated due to the high level of inter-individual and circadian variability. Recently, a dopamine-somatostatin chimera, BIM23B065, was under investigation to concurrently target the somatostatin and dopamine D2 receptors for the treatment of neuroendocrine tumors. However, both dopamine and somatostatin interact with different components of the cardiovascular system. This study established the response of the h...

Substituted anthraquinones represent a potential scaffold for DNA methyltransferase 1-specific inhibitors.

In humans, the most common epigenetic DNA modification is methylation of the 5-carbon of cytosines, predominantly in CpG dinucleotides. DNA methylation is an important epigenetic mark associated with gene repression. Disruption of the normal DNA methylation pattern is known to play a role in the initiation and progression of many cancers. DNA methyltransferase 1 (DNMT1), the most abundant DNA methyltransferase in humans, is primarily responsible for maintenance of the DNA methylation pattern and is consider...

Alternative conformations of a major antigenic site on RSV F.

The respiratory syncytial virus (RSV) fusion (F) glycoprotein is a major target of neutralizing antibodies arising from natural infection, and antibodies that specifically bind to the prefusion conformation of RSV F generally demonstrate the greatest neutralization potency. Prefusion-stabilized RSV F variants have been engineered as vaccine antigens, but crystal structures of these variants have revealed conformational differences in a key antigenic site located at the apex of the trimer, referred to as ant...

Angiotensin II Mediates the Axonal Trafficking of Tyrosine Hydroxylase and Dopamine β-Hydroxylase mRNAs and enhances Norepinephrine Synthesis in Primary Sympathetic Neurons.

In the sympatho-adrenal system, angiotensin II (Ang II) acts as a key neuromodulatory component. At sympathetic nerve terminals, Ang II influences sympathetic transmission by enhancing norepinephrine (NE) synthesis, facilitating NE release and inhibiting NE uptake. Previously, it was demonstrated that tyrosine hydroxylase (TH) mRNA is trafficked to the distal axons of primary superior cervical ganglia (SCG) neurons, directed by a cis-acting regulatory element (i.e. zipcode) located in the 3'UTR of the trans...

Characterization of the metabolite of AdipoRon in rat and human liver microsomes by ultra-high performance liquid chromatography combined with Q-Exactive Orbitrap tandem mass spectrometry.

AdipoRon is an orally active adiponectin receptor agonist. The aim of this study was to characterize the metabolites of AdipoRon in rat and human liver microsomes by using ultra-high performance liquid chromatography combined with Q-Exactive Orbitrap tandem mass spectrometry (UPLC-Q-Exactive-Orbitrap-MS) together with data processing techniques including extracted ion chromatograms and mass defect filter. AdipoRon (10 μM) was incubated with liver microsomes in the presence of NADPH and resulted in a total ...

Long-term Chemical Aging of Hybrid Halide Perovskites.

Since the power conversion efficiency (PCE) of hybrid halide perovskite solar cells (PSCs) could exceed 24%, extensive research has been focused on improving their long-term stability for commercialization in the near future. In a previous study, we reported that the addition of a certain amount of ionized iodide (triiodide: I3-) ions during the perovskite film formation significantly improved the efficiency of PSCs by reducing deep-level defects in the perovskite layer. Understanding the relationship betwe...

Injury Surveillance in Major League Soccer: A 4-Year Comparison of Injury on Natural Grass Versus Artificial Turf Field.

Artificial playing surfaces are becoming more common due to decreased cost of maintenance and increased field usability across different environmental conditions. The Fédération Internationale de Football Association (FIFA) has approved newer generation artificial turf for soccer competition at the elite level, but many elite-level athletes prefer to play on natural grass surfaces due to a perceived increase in injury rate, discomfort, and fatigability on artificial turf.

The Effects of Modulating Fundamental Frequency and Speech Rate on the Intelligibility, Communication Efficiency, and Perceived Naturalness of Synthetic Speech.

Purpose This study investigated how modulating fundamental frequency (f0) and speech rate differentially impact the naturalness, intelligibility, and communication efficiency of synthetic speech. Method Sixteen sentences of varying prosodic content were developed via a speech synthesizer. The f0 contour and speech rate of these sentences were altered to produce 4 stimulus sets: (a) normal rate with a fixed f0 level, (b) slow rate with a fixed f0 level, (c) normal rate with prosodically natural f0 variation,...

Filled Pauses as a Special Case of Automatic Speech Behaviors and the Effect of Parkinson's Disease.

Purpose In Parkinson's disease (PD), there are significant changes in the basal ganglia, a structure known to be important for controlling automatic responses to cues. Changes to the basal ganglia in PD impair an individual's ability to trigger a behavior in response to cues, but more so in response to internal cues more than external ones. Filled pauses are considered a subconscious or automatic speech response to an internal cue that there are difficulties with ongoing communication. Typical speakers use ...

High-content Analysis of Constitutive Androstane Receptor (CAR) Translocation Identifies Mosapride Citrate as a CAR Agonist that Represses Gluconeogenesis.

The constitutive androstane receptor (CAR) plays an important role in hepatic drug metabolism and detoxification but has recently been projected as a potential drug target for metabolic disorders due to its repression of lipogenesis and gluconeogenesis. Thus, identification of physiologically-relevant CAR modulators has garnered significant interest. Here, we adapted the previously characterized human CAR (hCAR) nuclear translocation assay in human primary hepatocytes (HPH) to a high-content format and scre...

Amygdala group II mGluRs mediate the inhibitory effects of systemic group II mGluR activation on behavior and spinal neurons in a rat model of arthritis pain.

The amygdala plays a critical role in emotional-affective aspects of behaviors and pain modulation. The central nucleus of amygdala (CeA) serves major output functions, and neuroplasticity in the CeA is linked to pain-related behaviors in different models. Activation of G-coupled group II metabotropic glutamate receptors (mGluRs), which consist of mGluR2 and mGluR3, can decrease neurotransmitter release and regulate synaptic plasticity. Group II mGluRs have emerged as targets for neuropsychiatric disorders ...

Identification of the amino acids in the Major Histocompatibility Complex class II region of Scottish Blackface sheep that are associated with resistance to nematode infection.

Lambs with the Major Histocompatibility Complex (MHC) DRB1*1101 allele have been shown to produce fewer nematode eggs following natural and deliberate infection. These sheep also possess fewer adult Teladorsagia circumcincta than sheep with alternative alleles at the DRB1 locus. However, it is unclear if this allele is responsible for the reduced egg counts or merely acts as a marker for a linked gene. This study defined the MHC haplotypes in a population of naturally infected Scottish Blackface sheep by PC...

Contribution of brown adipose tissue to human energy metabolism.

The present "obesogenic' environment has favored excessive energy intake resulting in the current obesity epidemic and its associated diseases. The epidemic has incentivized scientists to develop novel behavioral and pharmacological strategies that enhance energy expenditure to compensate for excessive energy intake. Although physical activity is effective to increase total energy expenditure, it is insufficient to induce negative energy balance and weight loss. With the discovery of brown adipose tissue (B...

Determination of the Crystal Structure and Substrate Specificity of Ananain.

Ananain (EC 3.4.22.31) accounts for less than 10% of the total enzyme in the crude pineapple stem extract known as bromelain, yet yields the majority of the proteolytic activity of bromelain. Despite a high degree of sequence identity between ananain and stem bromelain, the most abundant bromelain cysteine protease, ananain displays distinct chemical properties, substrate preference and inhibitory profile compared to stem bromelain. A tripeptidyl substrate library (REPLi) was used to further characterize th...

Oleanolic acid attenuates cisplatin-induced nephrotoxicity in mice and chemosensitizes human cervical cancer cells to cisplatin cytotoxicity.

Oleanolic acid (OA) is a natural triterpenoid that possesses numerous beneficial health effects such as antioxidant, anti-inflammatory and anti-apoptotic activities. In this study, we investigated the therapeutic effect of OA (10 and 40 mg/kg) on cisplatin (CP)-induced (13 mg/kg) nephrotoxicity. Treatment with OA 40 mg/kg once daily for 2 days, 48 h after CP-intoxication, ameliorated the increased serum markers and histological features of kidney injury. CP administration increased renal expression ...

Myo-inositol in the protection from cadmium-induced toxicity in mice kidney: An emerging nutraceutical challenge.

Cadmium (Cd) induces functional and morphological changes in kidney. Therefore, the effects of a natural nutraceutical antioxidant, myo-inositol (MI), were evaluated in mice kidneys after Cd challenge. Twenty-eight C57 BL/6 J mice were divided into these groups: 0.9% NaCl; MI (360 mg/kg/day); CdCl (2 mg/kg/day) plus vehicle; CdCl (2 mg/kg/day) plus MI (360 mg/kg/day). After 14 days, kidneys were processed for structural, biochemical and morphometric evaluation. Treatment with CdCl increased urea n...

Design and biological assessment of membrane-tethering neuroprotective peptides derived from the pituitary adenylate cyclase-activating polypeptide type 1 receptor.

The pituitary adenylate cyclase-activating polypeptide (PACAP) type 1 receptor (PAC1), a class B G protein-coupled receptor (GPCR), has emerged as a promising target for treating neurodegenerative conditions. Unfortunately, despite years of research, no PAC1-specific agonist has been discovered, as activity on two other GPCRs, VPAC1 and VPAC2, is retained with current analogs. Cell signaling is related to structural modifications in the intracellular loops (ICLs) of GPCRs. Thus, we hypothesized that peptide...

Natural Language Processing of Reddit Data to Evaluate Dermatology Patient Experiences and Therapeutics.

There is a lack of research studying patient-generated data on Reddit, one of the world's most popular forums with active users interested in dermatology. Techniques within natural language processing, a field of artificial intelligence, can analyze large amounts of text information and extract insights.

FSM: Fast and Scalable Network Motif Discovery for Exploring Higher-order Network Organizations.

Networks exhibit rich and diverse higher-order organizational structures. Network motifs, which are recurring significant patterns of inter-connections, are recognized as fundamental units to study the higher-order organizations of networks. However, the principle of selecting representative network motifs for local motif based clustering remains largely unexplored. We present a scalable algorithm called FSM for network motif discovery. FSM is advantageous in two-fold. First, it accelerates the motif discov...


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