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https://www.readbyqxmd.com/read/29786666/dopamine-receptor-subtypes-differentially-regulate-autophagy
#1
Dongmei Wang, Xinmiao Ji, Juanjuan Liu, Zhiyuan Li, Xin Zhang
Some dopamine receptor subtypes were reported to participate in autophagy regulation, but their exact functions and mechanisms are still unclear. Here we found that dopamine receptors D2 and D3 (D2-like family) are positive regulators of autophagy, while dopamine receptors D1 and D5 (D1-like family) are negative regulators. Furthermore, dopamine and ammonia, the two reported endogenous ligands of dopamine receptors, both can induce dopamine receptor internalization and degradation. In addition, we found that AKT (protein kinase B)-mTOR (mechanistic target of rapamycin) and AMPK (AMP-activated protein kinase) pathways are involved in DRD3 (dopamine receptor D3) regulated autophagy...
May 22, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29780355/therapeutic-interference-with-vascular-calcification-lessons-from-klotho-hypomorphic-mice-and-beyond
#2
REVIEW
Florian Lang, Christina Leibrock, Lisann Pelzl, Meinrad Gawaz, Burkert Pieske, Ioana Alesutan, Jakob Voelkl
Medial vascular calcification, a major pathophysiological process associated with cardiovascular disease and mortality, involves osteo-/chondrogenic transdifferentiation of vascular smooth muscle cells (VSMCs). In chronic kidney disease (CKD), osteo-/chondrogenic transdifferentiation of VSMCs and, thus, vascular calcification is mainly driven by hyperphosphatemia, resulting from impaired elimination of phosphate by the diseased kidneys. Hyperphosphatemia with subsequent vascular calcification is a hallmark of klotho-hypomorphic mice, which are characterized by rapid development of multiple age-related disorders and early death...
2018: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/29771914/regulation-of-vitamin-d-metabolizing-enzymes-in-murine-renal-and-extrarenal-tissues-by-dietary-phosphate-fgf23-and-1-25-oh-2d3
#3
Larissa Kägi, Carla Bettoni, Eva M Pastor-Arroyo, Udo Schnitzbauer, Nati Hernando, Carsten A Wagner
BACKGROUND: The 1,25-dihydroxyvitamin D3 (1,25(OH)2D3) together with parathyroid hormone (PTH) and fibroblast growth factor 23 (FGF23) regulates calcium (Ca2+) and phosphate (Pi) homeostasis, 1,25(OH)2D3 synthesis is mediated by hydroxylases of the cytochrome P450 (Cyp) family. Vitamin D is first modified in the liver by the 25-hydroxylases CYP2R1 and CYP27A1 and further activated in the kidney by the 1α-hydroxylase CYP27B1, while the renal 24-hydroxylase CYP24A1 catalyzes the first step of its inactivation...
2018: PloS One
https://www.readbyqxmd.com/read/29766000/vitamin-d3-induces-gene-expression-of-ox-ldl-scavenger-receptors-in-streptozotocin-induced-diabetic-rat-aortas-new-insight-into-the-role-of-vitamin-d-in-diabetic-atherosclerosis
#4
Shahab Alizadeh, Abbas Mirshafiey, Mahmoud Djalali, Ehsan Alvandi, Niyaz Mohammadzadeh Honarvar, Mohammad Hassan Javanbakht
Background: Several lines of evidence suggest that oxidized LDL (Ox-LDL) scavenger receptors play a crucial role in the genesis and progression of diabetic atherosclerosis. This study aimed to elucidate the effect of vitamin D3 on gene expression of lectin-like oxidized LDL receptor-1 (LOX-1), scavenger receptor-A (SR-A), Cluster of Differentiation 36 (CD36), and Cluster of Differentiation 68 (CD68) as the main Ox-LDL receptors in streptozotocin (STZ)-induced diabetic rat aortas. Methods: Eighteen Sprague-Dawley rats were randomly divided into three groups of six rats each...
April 2018: Reports of Biochemistry & Molecular Biology
https://www.readbyqxmd.com/read/29762856/vitamin-d-a-steroid-hormone-with-progesterone-like-activity
#5
G Monastra, S De Grazia, L De Luca, S Vittorio, V Unfer
OBJECTIVE: This review is aimed at demonstrating the progesterone-like activity exerted by the active form of vitamin D, or calcitriol (1,25(OH)2D). To achieve this outcome, we compared the effects in vivo and in vitro exerted by progesterone and vitamin D, with a special focus on the female reproductive system and pregnancy. MATERIALS AND METHODS: This is a literature review of the most important articles published in English on vitamin D as a hormone, mainly found by MEDLINE...
April 2018: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/29762475/growth-hormone-secretion-patterns-in-german-landrace-dl-fetuses-and-piglets-compared-to-dl-piglets-with-inherited-1-25-dihydroxyvitamin-d3-deficiency
#6
Manfred Mielenz, Michael W Pfaffl, Christina Schlumbohm, Johein Harmeyer, Nahid Parvizi
The regulation of growth hormone (GH) release during prenatal development and during early postnatal life is not entirely clarified. In this study plasma GH concentrations in pigs with inherited pseudo vitamin D deficiency type I (PDDR-I), which regularly show growth retardation, were compared during ontogeny with unaffected pigs of the same breed (German Landrace, DL) as control. Plasma GH concentrations were measured in plasma of chronically catheterized fetuses (beginning on day 101 after mating or after artificial insemination) and in piglets (day 37 postpartum (p...
May 15, 2018: Nutrients
https://www.readbyqxmd.com/read/29755397/stress-axis-regulation-by-vitamin-d-3-in-multiple-sclerosis
#7
Linda Rolf, Jan Damoiseaux, Inge Huitinga, Dorien Kimenai, Jody van den Ouweland, Raymond Hupperts, Joost Smolders
Introduction: Multiple sclerosis (MS) has been associated with both a poor vitamin D status and hyperactivity of the hypothalamus-pituitary-adrenal (HPA) axis. Since nuclear receptor ligands may regulate each other, we explored the association of vitamin D3 supplements with circadian cortisol levels in a double-blind and placebo-controlled supplementation study. Methods: Female patients with relapsing-remitting MS received vitamin D3 supplements (4,000 IU/day; n  = 22) or placebo ( n  = 19) during 16 weeks...
2018: Frontiers in Neurology
https://www.readbyqxmd.com/read/29754009/dietary-nitrogen-and-calcium-modulate-cyp27b1-expression-in-young-goats
#8
M R Wilkens, K Elfers, M Schmicke, G Breves, A S Muscher-Banse
In livestock, feeding a reduced nitrogen (N) diet is favored for economic and ecological reasons. Ruminants cope more easily with a reduced N diet than monogastric species. However, changes in mineral homeostasis such as a reduction in 1,25-dihydroxyvitamin D3 (1,25-(OH)2 D3 ) concentrations, calcium (Ca), and IGF1 levels were observed in goats kept on a reduced N diet. The decrease in 1,25-(OH)2 D3 occurred even during a simultaneous reduction in dietary N and Ca, whereas a solitary Ca reduction stimulated 1,25-(OH)2 D3 synthesis...
April 3, 2018: Domestic Animal Endocrinology
https://www.readbyqxmd.com/read/29753474/intramammary-25-hydroxyvitamin-d-3-treatment-modulates-innate-immune-responses-to-endotoxin-induced-mastitis
#9
Kathryn E Merriman, Jessi L Powell, Jose E P Santos, Corwin D Nelson
Vitamin D signaling in response to pathogen-associated molecules contributes to activation of innate immune responses of bovine monocytes. We hypothesized that lipopolysaccharide (LPS) of bacteria associated with mastitis in dairy cows activates the vitamin D pathway in innate immune cells of the udder and that increasing availability of 25-hydroxyvitamin D3 [25(OH)D3 ] would augment expression of vitamin D-associated genes. The objective of this experiment was to determine the effects of intramammary LPS and 25(OH)D3 treatments on activation of the vitamin D pathway and innate immune responses of mammary immune cells...
May 9, 2018: Journal of Dairy Science
https://www.readbyqxmd.com/read/29733645/aromatic-based-design-of-highly-active-and-noncalcemic-vitamin-d-receptor-agonists
#10
Pranjal Gogoi, Samuel Seoane, Rita Sigueiro, Thierry Guiberteau, Miguel A Maestro, Roman Perez-Fernandez, Natacha Rochel, Antonio Mouriño
1We report the design, synthesis, biological evaluation and structural analysis of a new class of vitamin D analogs that possess an aromatic m-phenylene D-ring and an alkyl chain replacing the C-ring. A key feature of the synthetic strategy is a stereoselective Pd-catalyzed construction of the triene system in aqueous medium that allows the rapid preparation of small amounts of VDR ligands for biological screening. Analogs with the shorter (2a) and longer (2d, 2e) side chains attached to the triene system have no calcemic activity...
May 7, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29733445/effects-of-treatment-with-an-angiotensin-2-receptor-blocker-and-or-vitamin-d3-on-parathyroid-hormone-and-aldosterone-a-randomized-placebo-controlled-trial
#11
Lise Sofie Bislev, Lene Langagergaard Rødbro, Jesper Nørgaard Bech, Erling Bjerregaard Pedersen, Lars Rolighed, Tanja Sikjaer, Lars Rejnmark
OBJECTIVE: Emerging evidence support a positive, bidirectional and clinical relevant interaction between parathyroid hormone (PTH) and the renin-angiotensin-aldosterone-system (RAAS). A beneficial effect of the widely used RAAS inhibitors might include a PTH lowering effect, as high PTH levels may be harmful to cardiovascular health. We aimed to investigate whether PTH levels are lowered by short-term treatment with an angiotensin 2 receptor blocker (valsartan) independently of co-administration of vitamin D3...
May 7, 2018: Clinical Endocrinology
https://www.readbyqxmd.com/read/29729086/the-novel-atypical-antipsychotic-cariprazine-demonstrates-dopamine-d-2-receptor-dependent-partial-agonist-actions-on-rat-mesencephalic-dopamine-neuronal-activity
#12
Sarah Delcourte, Charles R Ashby, Renaud Rovera, Béla Kiss, Nika Adham, Bence Farkas, Nasser Haddjeri
AIM: Cariprazine, a dopamine D3 -preferring D3 /D2 receptor partial agonist, is FDA approved for the treatment of schizophrenia and acute manic or mixed episodes of bipolar disorder. This study used in vivo electrophysiological techniques in anesthetized rats to determine cariprazine's effect on dopaminergic cell activity in the ventral tegmental area (VTA) and substantia nigra pars compacta (SNc). METHODS: Extracellular recordings of individual dopaminergic neurons were performed after oral or intravenous administration of cariprazine, the D3 receptor antagonist SB 277011A, the D2 receptor antagonist L741,626, and/or the D3 receptor agonist PD 128,907...
May 4, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29727000/rationally-designed-strigolactone-analogs-as-antagonists-of-the-d14-receptor
#13
Jun Takeuchi, Kai Jiang, Kei Hirabayashi, Yusaku Imamura, Yashan Wu, Yuqun Xu, Takuya Miyakawa, Hidemitsu Nakamura, Masaru Tanokura, Tadao Asami
Strigolactones (SLs) are plant hormones that inhibit shoot branching and act as signals in communications with symbiotic fungi and parasitic weeds in the rhizosphere. SL signaling is mediated by DWARF14 (D14), which is an α/β-hydrolase that cleaves SLs into an ABC tricyclic lactone and a butenolide group (i.e., D-ring). This cleavage reaction (hydrolysis and dissociation) is important for inducing the interaction between D14 and its target proteins, including D3 and D53. In this study, a hydrolysis-resistant SL analog was predicted to inhibit the activation of the D14 receptor, thereby disrupting the SL signaling pathway...
May 2, 2018: Plant & Cell Physiology
https://www.readbyqxmd.com/read/29725403/ron-is-overexpressed-in-bladder-cancer-and-contributes-to-tumorigenic-phenotypes-in-5637-cells
#14
Jun-Feng Chen, Bi-Xia Yu, Liang Ma, Xiu-Yi Lv, Jun-Hui Jiang, Qi Ma
Tyrosine kinase receptor macrophage stimulating 1 receptor (MST1R, also known as RON) contributes to the transformation and malignant progression observed in epithelial cells. The purpose of the present study is to assess the value of RON as a potential target in bladder cancer (BC) therapeutics. The expression profile of RON in BC tissues and adjacent noncancerous tissues was detected via immunohistochemistry. The rate of positive RON expression differed significantly between bladder urothelial cancer tissues (54...
May 2018: Oncology Letters
https://www.readbyqxmd.com/read/29722587/the-preclinical-discovery-and-development-of-cariprazine-for-the-treatment-of-schizophrenia
#15
Anna Wesołowska, Anna Partyka, Magdalena Jastrzębska-Więsek, Marcin Kołaczkowski
Cariprazine is approved in the United States and Europe for the treatment of manic or mixed episodes associated with bipolar I disorder and for the treatment of schizophrenia in adult patients. It is typically administered orally once a day (a dose range 1.5 - 6 mg/day), does require titration, and may be given with or without food. It has a half-life of 2 - 4 days with an active metabolite that has a terminal half-life of 2 - 3 weeks. Areas covered: This review article focuses on the preclinical discovery of cariprazine providing details regarding its pharmacological, behavioral, and neurochemical mechanisms and its contribution to clinical therapeutic benefits...
May 3, 2018: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/29720711/in-vitro-and-in-vivo-characterization-of-pcc0104005-a-novel-modulator-of-serotonin-dopamine-activity-as-an-atypical-antipsychotic-drug
#16
Yanan Xu, Xiaoyin Zhu, Hongbo Wang, Shanyue Sun, Xin Yue, Jingwei Tian
PCC0104005 is a novel drug candidate for treating schizophrenia that displays high affinity for serotonin, dopamine, and noradrenaline receptors, including partial agonism at dopamine D2 , D3 , D4 , serotonin 5-HT1A , and 5-HT2A receptors and antagonism at 5-HT2B , 5-HT6 , and 5-HT7 receptors. PCC0104005 blocks MK-801-induced hyperactivity in rats, consistent with the reduction in dopamine D2 receptor stimulation and increased dopamine release in the medial prefrontal cortex. PCC0104005 inhibits 5-HTP-induced head twitches in rats, due to its moderate affinity for human 5-HT2A receptors (Ki = 5...
May 2, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29719203/the-burgeoning-role-of-cytochrome-p450-mediated-vitamin-d-metabolites-against-colorectal-cancer
#17
REVIEW
Peili Wang, Xuan Qin, Mingyao Liu, Xin Wang
The metabolites of vitamin D3 (VD3) mediated by different cytochrome P450 (CYP) enzymes, play fundamental roles in many physiological processes in relation to human health. These metabolites regulate a variety of cellular signal pathways through the direct binding of activated vitamin D receptor/retinoic X receptor (VDR/RXR) heterodimeric complex to specific DNA sequences. Thus, the polymorphisms of VDR and VD3 metabolizing enzymes lead to differentiated efficiency of VD3 and further affect serum VD3 levels...
April 30, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29718408/ancient-nuclear-receptor-vdr-with-new-functions-microbiome-and-inflammation
#18
Danika Bakke, Jun Sun
The biological functions of 1α,25-dihydroxyvitamin D3 are regulated by nuclear receptor vitamin D receptor (VDR). The expression level of VDR is high in intestine. VDR is an essential regulator of intestinal cell proliferation, barrier function, and immunity. Vitamin D/VDR plays a protective role in inflammatory bowel diseases (IBDs), both ulcerative colitis and Crohn's disease. Emerging evidence demonstrates low VDR expression and dysfunction of vitamin D/VDR signaling in patients with IBD. Here, we summarize the progress made in vitamin D/VDR signaling in genetic regulation, immunity, and the microbiome in IBD...
April 28, 2018: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/29715698/antenatal-vitamin-d-preserves-placental-vascular-and-fetal-growth-in-experimental-chorioamnionitis-due-to-intra-amniotic-endotoxin-exposure
#19
Michael W Cookson, Sharon L Ryan, Gregory J Seedorf, R Blair Dodson, Steve H Abman, Erica W Mandell
BACKGROUND:  Chorioamnionitis (CA) is associated with a high risk for the development of bronchopulmonary dysplasia (BPD) after preterm birth, but mechanisms that increase susceptibility for BPD and strategies to prevent BPD are uncertain. As a model of CA, antenatal intra-amniotic (IA) endotoxin (ETX) exposure alters placental structure, causes fetal growth restriction, increases perinatal mortality, and causes sustained cardiorespiratory abnormalities throughout infancy. Vitamin D (Vit D) has been shown to have both anti-inflammatory and proangiogenic properties...
May 1, 2018: American Journal of Perinatology
https://www.readbyqxmd.com/read/29710404/design-synthesis-and-biological-evaluation-of-structurally-constrained-hybrid-analogues-containing-ropinirole-moiety-as-a-novel-class-of-potent-and-selective-dopamine-d3-receptor-ligands
#20
Benhua Zhou, Kwon Ho Hong, Min Ji, Jin Cai
Two series of hybrid analogues were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine D3 receptor. Binding affinities of target compounds were determined (using the method of radioligand binding assay). Compared to comparator agent BP897, compounds 2a and 2c were found to demonstrate a considerable binding affinity and selectivity for D3 receptor, and especially compound 2h was similarly potent and more selective D3R ligand than BP897, a positive reference. Thus they may provide valuable information for the discovery and development of highly potent dopamine D3 receptor ligands with outstanding selectivity...
April 30, 2018: Chemical Biology & Drug Design
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