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https://www.readbyqxmd.com/read/28324061/progesterone-protects-against-bpa-induced-arrhythmias-in-female-rat-cardiac-myocytes-via-rapid-signaling
#1
Jianyong Ma, Kui Hong, Hong-Sheng Wang
Bisphenol A (BPA) is an estrogenic endocrine disrupting chemical (EDC) that has a range of potential adverse health effects. Previously we showed that acute exposure to BPA promoted arrhythmias in female rat hearts through estrogen receptor rapid signaling. Progesterone (P4) and estrogen have antagonistic or complementary actions in a number of tissues and systems. In the current study, we examined the influence, and possible protective effect, of P4 on the rapid cardiac actions of BPA in female rat cardiac myocytes...
January 25, 2017: Endocrinology
https://www.readbyqxmd.com/read/28324026/gonadotropin-inhibitory-hormone-gnih-the-piscine-ortholog-of-lpxrfa-participates-in-17%C3%AE-estradiol-feedback-in-female-goldfish-reproduction
#2
Xin Qi, Wenyi Zhou, Qingqing Wang, Liang Guo, Danqi Lu, Haoran Lin
Gonadotropin-inhibitory hormone (GnIH) plays a critical role in regulating GnRH, GtH and steroidogenesis in teleosts. In the present study, we sought to determine whether E2 (17β-estradiol) acts directly on GnIH neurons to regulate reproduction in goldfish, a seasonal breeder, and we investigated the role of estrogen receptors in mediating this process. We found that GnIH neurons co-express three types of ERs. Ovariectomy and letrozole implantation into female goldfish at the vitellogenic stage elicited a significant decrease in the expression of GnIH mRNA, and E2 supplementation abolished this effect...
January 4, 2017: Endocrinology
https://www.readbyqxmd.com/read/28323850/ligand-guided-homology-modelling-of-the-gabab2-subunit-of-the-gabab-receptor
#3
Thibaud Freyd, Dawid Warszycki, Stefan Mordalski, Andrzej J Bojarski, Ingebrigt Sylte, Mari Gabrielsen
γ-aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the central nervous system, and disturbances in the GABAergic system have been implicated in numerous neurological and neuropsychiatric diseases. The GABAB receptor is a heterodimeric class C G protein-coupled receptor (GPCR) consisting of GABAB1a/b and GABAB2 subunits. Two GABAB receptor ligand binding sites have been described, namely the orthosteric GABA binding site located in the extracellular GABAB1 Venus fly trap domain and the allosteric binding site found in the GABAB2 transmembrane domain...
2017: PloS One
https://www.readbyqxmd.com/read/28320163/inhibition-of-17-beta-estradiol-on-neuronal-excitability-via-enhancing-girk1-mediated-inwardly-rectifying-potassium-currents-and-girk1-expression
#4
Yuwen Zhang, Yian Huang, Guoxiang Wang, Xin Wang, Yun Wang
BACKGROUND: Catamenial epilepsy is a common central nervous system disease in female, which is influenced by the 17-β-estradiol (estrogen) level during the menstrual cycle. Low level (<0.05ng/ml) of estrogen normally accompanies with the perimenstrual classification of catamenial epilepsy, however, without clear mechanism. In previous studies, estrogen has been demonstrated to possess widely regulatory effects on potassium channels. Here, the effect of 17-β-estradiol on modulating inwardly rectifying K(+) (Kir) currents was investigated in cultured hippocampal neurons...
April 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28319060/the-anti-diabetic-drug-exenatide-a-glucagon-like-peptide-1-receptor-agonist-counteracts-hepatocarcinogenesis-through-camp-pka-egfr-stat3-axis
#5
M Zhou, M T S Mok, H Sun, A W Chan, Y Huang, A S L Cheng, G Xu
Epidemiological studies have demonstrated a close association of type 2 diabetes and hepatocellular carcinoma (HCC). Exenatide (Ex-4), a potent diabetes drug targeting glucagon-like peptide-1 receptor (GLP-1R), is protective against non-alcoholic fatty liver disease (NAFLD). However, the Ex-4 function and GLP-1R status have yet been explored in HCC. Herein we investigated the effect of Ex-4 in diethylnitrosamine (DEN)-treated mice consuming control or high-fat high-carbohydrate diet. Administration of Ex-4 significantly improved obesity-induced hyperglycemia and hyperlipidemia and reduced HCC multiplicity in obese DEN-treated mice, in which suppressed proliferation and induced apoptosis were confined to tumor cells...
March 20, 2017: Oncogene
https://www.readbyqxmd.com/read/28318945/identification-and-structure-activity-relationships-of-quinoline-tertiary-alcohol-modulators-of-ror%C3%AE-t
#6
David A Kummer, Maxwell D Cummings, Marta Abad, Joseph Barbay, Glenda Castro, Ronald Wolin, Kevin D Kreutter, Umar Maharoof, Cynthia Milligan, Rachel Nishimura, Joan Pierce, Celine Schalk-Hihi, John Spurlino, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Craig Woods, Xiaohua Xue, James P Edwards, Anne M Fourie, Kristi Leonard
A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity relationships and structure-based drug design methods led to the discovery of a series of modulators with improved RORγt inhibitory potency and inverse agonism properties.
February 21, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28318299/lithocholic-acid-a-new-emergent-protector-of-intestinal-calcium-absorption-under-oxidant-conditions
#7
Ana M Marchionatti, Adriana Pérez, María A Rivoira, Valeria A Rodríguez, Nori G Tolosa de Talamoni
LCA and 1,25(OH)2D3 are vitamin D receptor ligands with different binding affinity. The secosteroid stimulates intestinal Ca(2+) absorption. Whether LCA alters this process remains unknown. The aim of our work was to determine the effect of LCA on intestinal Ca(2+) absorption in the absence or presence of NaDOC, bile acid that inhibits the cation transport. The data show that LCA by itself did not alter intestinal Ca(2+) absorption, but prevented the inhibitory effect of NaDOC. The concomitant administration of LCA avoided the reduction of intestinal alkaline phosphatase activity caused by NaDOC...
March 20, 2017: Biochemistry and Cell Biology, Biochimie et Biologie Cellulaire
https://www.readbyqxmd.com/read/28315687/-10-gingerol-a-major-phenolic-constituent-of-ginger-root-induces-cell-cycle-arrest-and-apoptosis-in-triple-negative-breast-cancer-cells
#8
Megan M Bernard, Jason R McConnery, David W Hoskin
The ginger rhizome is rich in bioactive compounds, including [6]-gingerol, [8]-gingerol, and [10]-gingerol; however, to date, most research on the anti-cancer activities of gingerols have focused on [6]-gingerol. In this study, we compared [10]-gingerol with [8]-gingerol and [6]-gingerol in terms of their ability to inhibit the growth of human and mouse mammary carcinoma cells. A colorimetric assay based on the enzymatic reduction of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide revealed that [10]-gingerol was more potent than [6]-gingerol and at least as potent as [8]-gingerol for the inhibition of triple-negative human (MDA-MB-231, MDA-MB-468) and mouse (4T1, E0771) mammary carcinoma cell growth...
March 15, 2017: Experimental and Molecular Pathology
https://www.readbyqxmd.com/read/28315344/further-analysis-of-the-inhibition-by-agmatine-on-the-cardiac-sympathetic-outflow-role-of-the-%C3%AE-2-adrenoceptor-subtypes
#9
Luis Cobos-Puc, Hilda Aguayo-Morales, Janeth Ventura-Sobrevilla, Diana Luque-Contreras, Miguel Chin-Chan
This study has investigated the role of the α2-adrenoceptor subtypes involved in the inhibition of the cardiac sympathetic outflow induced by intravenous (i.v) infusions of agmatine. Therefore, we analysed the effect of an i.v. bolus injections of the selective antagonists BRL 44408 (300μg/kg; α2A), imiloxan (3000μg/kg; α2B), and JP-1302 (300μg/kg; α2C) given separately, and their combinations: BRL 44408 plus Imiloxan, JP 1302 plus imiloxan, BRL 44408 plus JP-1302, BRL 44408 plus imiloxan plus JP-1302 on the cardiac sympatho-inhibition of agmatine...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315335/microrna-99a-inhibits-insulin-induced-proliferation-migration-dedifferentiation-and-rapamycin-resistance-of-vascular-smooth-muscle-cells-by-inhibiting-insulin-like-growth-factor-1-receptor-and-mammalian-target-of-rapamycin
#10
Zi-Wei Zhang, Rui-Wei Guo, Jin-Lin Lv, Xian-Mei Wang, Jin-Shan Ye, Ni-Hong Lu, Xing Liang, Li-Xia Yang
Patients with type 2 diabetes mellitus (T2DM) are characterized by insulin resistance and are subsequently at high risk for atherosclerosis. Hyperinsulinemia has been associated with proliferation, migration, and dedifferentiation of vascular smooth muscle cells (VSMCs) during the pathogenesis of atherosclerosis. Moreover, insulin-like growth factor-1 receptor (IGF-1R) and mammalian target of rapamycin (mTOR) have been demonstrated to be the underlying signaling pathways. Recently, microRNA-99a (miR-99a) has been suggested to regulate the phenotypic changes of VSMCs in cancer cells...
March 15, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28314274/increased-hgf-expression-induces-resistance-to-c-met-tyrosine-kinase-inhibitors-in-gastric-cancer
#11
So Yeong Ahn, Jin Kim, Min A Kim, Jiwoon Choi, Woo Ho Kim
BACKGROUND: Increased expression of hepatocyte growth factor (HGF) and MET proto-oncogene (c-MET) is associated with poor prognosis in various cancer types. Recently, it was reported that the expression of HGF induces resistance to tyrosine kinase inhibitors (TKIs) targeting epidermal growth factor receptor, human epidermal receptor receptor 2, and b-raf proto-oncogene. Here, we investigated the effects of HGF overexpression in gastric cancer cells in the absence or presence of c-MET TKIs...
March 2017: Anticancer Research
https://www.readbyqxmd.com/read/28314159/aging-alters-the-molecular-dynamics-of-synapses-in-a-sexually-dimorphic-pattern-in-zebrafish-danio-rerio
#12
Elif Tugce Karoglu, Dilara Ozge Halim, Bahriye Erkaya, Ferda Altaytas, Ayca Arslan-Ergul, Ozlen Konu, Michelle M Adams
The zebrafish has become a popular model for studying normal brain aging due to its large fecundity, conserved genome, and available genetic tools; but little data exists about neurobiological age-related alterations. The current study tested the hypothesis of an association between brain aging and synaptic protein loss across males and females. Western blot analysis of synaptophysin (SYP), a presynaptic vesicle protein, and postsynaptic density-95 (PSD-95) and gephyrin (GEP), excitatory and inhibitory postsynaptic receptor-clustering proteins, respectively, was performed in young, middle-aged, and old male and female zebrafish (Danio rerio) brains...
February 20, 2017: Neurobiology of Aging
https://www.readbyqxmd.com/read/28306571/cns-syndromes-associated-with-antibodies-against-metabotropic-receptors
#13
Eric Lancaster
PURPOSE OF REVIEW: Autoantibodies to Central nervous system (CNS) metabotropic receptors are associated with a growing family of autoimmune brain diseases, including encephalitis, basal ganglia encephalitis, Ophelia syndrome, and cerebellitis. The purpose of this review is to summarize the state of knowledge regarding the target receptors, the neurological autoimmune disorders, and the pathogenic mechanisms. RECENT FINDINGS: Antibodies to the γ-aminobutyric acid B receptor are associate with limbic encephalitis and severe seizures, often with small cell lung cancers...
March 16, 2017: Current Opinion in Neurology
https://www.readbyqxmd.com/read/28306177/frequency-and-functional-characterization-of-exhausted-cd8-t-cells-in-chronic-lymphocytic-leukemia
#14
Saeid Taghiloo, Esmaeil Allahmoradi, Mohsen Tehrani, Hadi Hossein-Nataj, Ramin Shekarriz, Ghasem Janbabaei, Saeid Abediankenari, Hossein Asgarian-Omran
OBJECTIVES: The phenotypic and functional properties of Tim-3+/PD-1+/CD8+ cells as exhausted T-cells were investigated in chronic lymphocytic leukemia (CLL). METHODS: Frequency of CD8+/Tim-3+/PD-1+ exhausted cells was determined by flow cytometry. For functional analysis, magnetic beads isolated CD8+ T-cells were stimulated with PHA and PMA/ionocymin to assess their proliferative responses and cytokine production by MTT and ELISA, respectively. Cytotoxic activity of isolated CD8+ T-cells was determined using CD107a degranulation assay...
March 17, 2017: European Journal of Haematology
https://www.readbyqxmd.com/read/28303937/vitamin-d-inhibits-lymphangiogenesis-through-vdr-dependent-mechanisms
#15
Saleh Yazdani, Fariba Poosti, Luis Toro, Johannes Wedel, Rik Mencke, Katarina Mirković, Martin H de Borst, J Steven Alexander, Gerjan Navis, Harry van Goor, Jacob van den Born, Jan-Luuk Hillebrands
Excessive lymphangiogenesis is associated with cancer progression and renal disease. Attenuation of lymphangiogenesis might represent a novel strategy to target disease progression although clinically approved anti-lymphangiogenic drugs are not available yet. VitaminD(VitD)-deficiency is associated with increased cancer risk and chronic kidney disease. Presently, effects of VitD on lymphangiogenesis are unknown. Given the apparently protective effects of VitD and the deleterious associations of lymphangiogenesis with renal disease, we here tested the hypothesis that VitD has direct anti-lymphangiogenic effects in vitro and is able to attenuate lymphangiogenesis in vivo...
March 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28303403/hypocretin-orexin-and-plastic-adaptations-associated-with-drug-abuse
#16
Corey Baimel, Stephanie L Borgland
Dopamine neurons in the ventral tegmental area (VTA) are a critical part of the neural circuits that underlie reward learning and motivation. Dopamine neurons send dense projections throughout the brain and recent observations suggest that both the intrinsic properties and the functional output of dopamine neurons are dependent on projection target and are subject to neuromodulatory influences. Lateral hypothalamic hypocretin (also termed orexin) neurons project to the VTA and contain both hypocretin and dynorphin peptides in the same dense core vesicles suggesting they may be co-released...
March 17, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28303303/melatonin-signalling-and-type-2-diabetes-risk-too-little-too-much-or-just-right
#17
EDITORIAL
Hindrik Mulder
Of the associations of genetic variants with type 2 diabetes, the one of an SNP in an intron of the gene encoding the melatonin receptor 1B (MTNR1B) has been remarkably robust. Work from our group and others has provided support for a model where carriers of this risk G allele exhibit increased MTNR1B expression in islets of Langerhans. Most published studies to date favour that melatonin's action on the beta cell is inhibition of insulin secretion. Hence, our model proposes that this inhibitory effect of melatonin is exaggerated in carriers of the MTNR1B risk G allele...
March 16, 2017: Diabetologia
https://www.readbyqxmd.com/read/28303296/sortase-a-aided-escherichia-coli-expression-system-for-functional-osteoprotegerin-cysteine-rich-domain
#18
Mengmeng Jin, Yuan Chen, Yunfeng Zhao, Luyang Che, Yanyan Ma, Jingzhe Li, Yi Wang, Hua Tao, Juan Ma, Bing Pan, Changzhen Liu, Peng Huang
As a natural inhibitor of the receptor activator of nuclear factor-кB ligand (RANKL), osteprotegerin (OPG) is considered a promising treatment for metabolic bone diseases. Typical approaches for preparing recombinant OPG or its derivatives employ eukaryotic expression systems. Due to the advantages of a prokaryotic expression system, which include its convenience, low cost, and abundant production, in this study, we establish a strategy for preparing functional OPG using the Escherichia coli expression system...
March 16, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28303090/the-inhibitory-effect-of-%C3%AE-%C3%AE-hydrolase-domain-containing-6-abhd6-on-the-surface-targeting-of-glua2-and-glua3-containing-ampa-receptors
#19
Mengping Wei, Moye Jia, Jian Zhang, Lulu Yu, Yunzhi Zhao, Yingqi Chen, Yimeng Ma, Wei Zhang, Yun S Shi, Chen Zhang
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptors (AMPARs) are major excitatory receptors that mediate fast neurotransmission in the mammalian brain. The surface expression of functional AMPARs is crucial for synaptic transmission and plasticity. AMPAR auxiliary subunits control the biosynthesis, membrane trafficking, and synaptic targeting of AMPARs. Our previous report showed that α/β-hydrolase domain-containing 6 (ABHD6), an auxiliary subunit for AMPARs, suppresses the membrane delivery and function of GluA1-containing receptors in both heterologous cells and neurons...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28302446/electrophysiological-evidence-of-increased-glycine-receptor-mediated-phasic-and-tonic-inhibition-by-blockade-of-glycine-transporters-in-spinal-superficial-dorsal-horn-neurons-of-adult-mice
#20
Misa Oyama, Seiya Kuraoka, Shun Watanabe, Takashi Iwai, Mitsuo Tanabe
To understand the synaptic and/or extrasynaptic mechanisms underlying pain relief by blockade of glycine transporter subtypes GlyT1 and GlyT2, whole-cell recordings were made from dorsal horn neurons in spinal slices from adult mice, and the effects of NFPS and ALX-1393, selective GlyT1 and GlyT2 inhibitors, respectively, on phasic evoked or miniature glycinergic inhibitory postsynaptic currents (eIPSCs or mIPSCs) were examined. NFPS and ALX-1393 prolonged the decay phase of eIPSCs without affecting their amplitude...
February 27, 2017: Journal of Pharmacological Sciences
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