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Retinoid X Receptor

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https://www.readbyqxmd.com/read/28089347/virtual-screening-and-experimental-validation-identify-novel-modulators-of-nuclear-receptor-rxr%C3%AE-from-drugbank-database
#1
Dan Xu, Lijun Cai, Shangjie Guo, Lei Xie, Meimei Yin, Ziwen Chen, Hu Zhou, Ying Su, Zhiping Zeng, Xiaokun Zhang
Retinoid X receptor alpha (RXRα), an important ligand-dependent transcription factor, plays a critical role in the development of various cancers and metabolic and neurodegenerative diseases. Therefore, RXRα represents one of the most important targets in modern drug discovery. In this study, Drugbank 2.0 with 1280 old drugs were virtually screened by Glide according to the crystal structure of ligand-binding domain (LBP) of RXRα. 15 compounds selected were tested for their binding and transcriptional activity toward RXRα by Biacore and reporter gene assay, respectively...
December 26, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28088372/nanoformulation-of-dual-bexarotene-tailed-phospholipid-conjugate-with-high-drug-loading
#2
Ruiyu He, Yawei Du, Longbing Ling, Muhammad Ismail, Yongpeng Hou, Chen Yao, Xinsong Li
Bexarotene (Bex), a synthetic retinoid X receptor-selective activator, has been proved to be an efficacious chemotherapeutic agent. But, its clinical application is limited due to the poor solubility. In this report, dual bexarotene-tailed phospholipid (DBTP) conjugate based nanovesicles were prepared in order to develop new nanoformulation. DBTP conjugate was first synthesized by conjugating two Bex molecules with glycerophosphorylcholine (GPC) through facial esterification. The amphiphilic DBTP nanovesicles were prepared without any additive by reverse-phase evaporation method...
January 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28069388/vitamin-d-receptor-deficit-induces-activation-of-renin-angiotensin-system-via-sirt1-modulation-in-podocytes
#3
Nirupama Chandel, Kamesh Ayosolla, Hongxiu Wen, Xiqian Lan, Shabirul Haque, Moin A Saleem, Ashwani Malhotra, Pravin C Singhal
Vitamin D receptor (VDR) deficient status has been shown to be associated with the activation of renin angiotensin system (RAS). We hypothesized that lack of VDR would enhance p53 expression in podocytes through down regulation of SIRT1; the former would enhance the transcription of angiotensinogen (Agt) and angiotensinogen II type 1 receptor (AT1R) leading to the activation of RAS. Renal tissues of VDR mutant (M) mice displayed increased expression of p53, Agt, renin, and AT1R. In vitro studies, VDR knockout podocytes not only displayed up regulation p53 but also displayed enhanced expression of Agt, renin and AT1R...
January 6, 2017: Experimental and Molecular Pathology
https://www.readbyqxmd.com/read/28054069/challenge-and-perspective-the-relevance-of-ultraviolet-uv-radiation-and-the-vitamin-d-endocrine-system-vdes-for-psoriasis-and-other-inflammatory-skin-diseases
#4
Jörg Reichrath, Roman Saternus, Thomas Vogt
During evolution, the ability of many organisms to synthesize vitamin D photochemically represented, and still represents, a major driving factor for the development of life on earth. In humans because not more than 10-20% of the requirement of vitamin D can be satisfied by the diet (under most living conditions in the US and Europe), the remaining 80-90% need to be photochemically synthesized in the skin through the action of solar or artificial ultraviolet-B (UV-B) radiation. The skin is a key organ of the human body's vitamin D endocrine system (VDES), representing both the site of vitamin D synthesis and a target tissue for biologically active vitamin D metabolites...
January 5, 2017: Photochemical & Photobiological Sciences
https://www.readbyqxmd.com/read/28041731/analysis-of-bull-bos-taurus-seminal-vesicle-fluid-proteome-in-relation-to-seminal-plasma-proteome
#5
B Westfalewicz, M A Dietrich, A Mostek, A Partyka, W Bielas, W Niżański, A Ciereszko
The existing knowledge on the bull seminal vesicle proteome, a major seminal plasma constituent, and its relationship with seminal plasma is limited. This knowledge is prerequisite for a better understanding of seminal plasma variability, which is linked to semen quality. The objective of this study was to characterize the proteomes of seminal vesicle fluid and seminal plasma and to compare them to better understand the origin of seminal plasma proteins. We collected ejaculates and seminal vesicle fluid postmortem from 6 mature Holstein Friesian bulls...
December 29, 2016: Journal of Dairy Science
https://www.readbyqxmd.com/read/28007475/mechanisms-of-retinoic-acid-signaling-during-cardiogenesis
#6
REVIEW
Sonia Stefanovic, Stéphane Zaffran
Substantial experimental and epidemiological data have highlighted the interplay between nutritional and genetic factors in the development of congenital heart defects. Retinoic acid (RA), a derivative of vitamin A, plays a key role during vertebrate development including the formation of the heart. Retinoids bind to RA and retinoid X receptors (RARs and RXRs) which then regulate tissue-specific genes. Here, we will focus on the roles of RA signaling and receptors in gene regulation during cardiogenesis, and the consequence of deregulated retinoid signaling on heart formation and congenital heart defects...
December 19, 2016: Mechanisms of Development
https://www.readbyqxmd.com/read/28003731/a-regulatory-sequence-from-the-retinoid-x-receptor-%C3%AE-gene-directs-expression-to-horizontal-cells-and-photoreceptors-in-the-embryonic-chicken-retina
#7
Maria K E Blixt, Finn Hallböök
PURPOSE: Combining techniques of episomal vector gene-specific Cre expression and genomic integration using the piggyBac transposon system enables studies of gene expression-specific cell lineage tracing in the chicken retina. In this work, we aimed to target the retinal horizontal cell progenitors. METHODS: A 208 bp gene regulatory sequence from the chicken retinoid X receptor γgene (RXRγ208) was used to drive Cre expression. RXRγ is expressed in progenitors and photoreceptors during development...
2016: Molecular Vision
https://www.readbyqxmd.com/read/27993043/mechanisms-of-action-of-compounds-that-enhance-storage-lipid-accumulation-in-daphnia-magna
#8
Rita Jordão, Bruno Campos, Benjamín Piña, Romà Tauler, Amadeu M V M Soares, Carlos Barata
Accumulation of storage lipids in the crustacean Daphnia magna can be altered by a number of exogenous and endogenous compounds, like 20-hydroxyecdysone (natural ligand of the ecdysone receptor, EcR), methyl farnesoate, pyrirproxyfen (agonists of the methyl farnesoate receptor, MfR), and tributyltin (agonist of the retinoid X acid receptor, RXR). This effect, analogous to the obesogenic disruption in mammals, alters Daphnia's growth and reproductive investment. Here we propose that storage lipid accumulation in droplets is regulated in Daphnia by the interaction between the nuclear receptor heterodimer EcR:RXR and MfR...
December 20, 2016: Environmental Science & Technology
https://www.readbyqxmd.com/read/27966173/development-of-a-magnetic-microbead-affinity-selection-screen-magmass-using-mass-spectrometry-for-ligands-to-the-retinoid-x-receptor-%C3%AE
#9
Michael D Rush, Elisabeth M Walker, Gerd Prehna, Tristesse Burton, Richard B van Breemen
To overcome limiting factors in mass spectrometry-based screening methods such as automation while still facilitating the screening of complex mixtures such as botanical extracts, magnetic microbead affinity selection screening (MagMASS) was developed. The screening process involves immobilization of a target protein on a magnetic microbead using a variety of possible chemistries, incubation with mixtures of molecules containing possible ligands, a washing step that removes non-bound compounds while a magnetic field retains the beads in the microtiter well, and an organic solvent release step followed by LC-MS analysis...
December 13, 2016: Journal of the American Society for Mass Spectrometry
https://www.readbyqxmd.com/read/27940374/inhibitory-effect-of-pcsk9-on-abca1-protein-expression-and-cholesterol-efflux-in-macrophages
#10
Maria Pia Adorni, Eleonora Cipollari, Elda Favari, Ilaria Zanotti, Francesca Zimetti, Alberto Corsini, Chiara Ricci, Franco Bernini, Nicola Ferri
BACKGROUND AND AIMS: Proprotein convertase subtilisin/kexin type 9 (PCSK9) may have extra-hepatic effects on cholesterol homeostasis of vascular macrophages. In this study, we aimed to investigate PCSK9 role on the anti-atherogenic process of ATP binding cassette transporter A1 (Abca1)-mediated cholesterol efflux. METHODS: Abca1-mediated cholesterol efflux was evaluated by a radioisotopic technique in mouse peritoneal macrophages (MPM) from wild-type (WT) or LDL receptor knock-out (Ldlr(-/-)) mice exposed to human recombinant PCSK9, in the presence of liver X receptor/retinoid X receptor (LXR/RXR) ligands or acetylated LDL (AcLDL) to stimulate Abca1 expression...
November 16, 2016: Atherosclerosis
https://www.readbyqxmd.com/read/27922847/apolipoprotein-e-metabolism-and-functions-in-brain-and-its-role-in-alzheimer-s-disease
#11
Fan Liao, Hyejin Yoon, Jungsu Kim
PURPOSE OF REVIEW: APOE4 genotype is the strongest genetic risk factor for Alzheimer's disease. Prevailing evidence suggests that amyloid β plays a critical role in Alzheimer's disease. The objective of this article is to review the recent findings about the metabolism of apolipoprotein E (ApoE) and amyloid β and other possible mechanisms by which ApoE contributes to the pathogenesis of Alzheimer's disease. RECENT FINDINGS: ApoE isoforms have differential effects on amyloid β metabolism...
February 2017: Current Opinion in Lipidology
https://www.readbyqxmd.com/read/27919949/1%C3%AE-dihydroxyvitamin-d3-and-retinoic-acid-increase-nuclear-vitamin-d-receptor-expression-in-monocytic-thp-1-cells
#12
Hikaru Uchida, Yuichiro Hasegawa, Hiromichi Takahashi, Makoto Makishima
BACKGROUND: 1α,25-Dihydroxyvitamin D3 [1,25(OH)2D3] and retinoic acid, such as all-trans retinoic acid (ATRA) and 9-cis retinoic acid (9cRA), are known to induce differentiation of myeloid leukemia cells. Combined treatment effectively enhances the differentiation effect, particularly in monocytic leukemia cells. The underlying mechanism of this combined effect remains unknown. MATERIALS AND METHODS: THP-1 monocytic leukemia cells were treated with 1,25(OH)2D3 in combination with 9cRA, ATRA or selective synthetic ligand for retinoic acid receptor (RAR) or retinoid X receptor (RXR), and the nuclear expression and function of vitamin D receptor (VDR) were examined...
2016: Anticancer Research
https://www.readbyqxmd.com/read/27916310/effects-of-chronic-dietary-exposure-of-zinc-oxide-nanoparticles-on-the-serum-protein-profile-of-juvenile-common-carp-cyprinus-carpio-l
#13
Latifeh Chupani, Eliška Zusková, Hamid Niksirat, Aleš Panáček, Vanessa Lünsmann, Sven-Bastiaan Haange, Martin von Bergen, Nico Jehmlich
Zinc oxide (ZnO) nanoparticles (NPs) have been dramatically used in industry, biology, and medicine. Despite their interesting physico-chemical properties for application in various industrial, medical, and consumer products, safe use of ZnO NPs are under challenges due to the inadequate information related to their toxicological endpoints. Proteomics was applied to evaluate the sub-lethal effects of dietary exposure to ZnO NPs on serum proteome profile of juvenile common carp, (Cyprinus carpio). Therefore, ZnO NPs solution (500mgkg(-1) of feed) was added to a commercial carp feed for six weeks...
February 1, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/27890585/cadmium-in%C3%A2-vivo-exposure-alters-stress-response-and-endocrine-related-genes-in-the-freshwater-snail-physa-acuta-new-biomarker-genes-in-a-new-model-organism
#14
Pedro Martínez-Paz, Mónica Morales, Paloma Sánchez-Argüello, Gloria Morcillo, José Luis Martínez-Guitarte
The freshwater snail Physa acuta is a sensitive organism to xenobiotics that is appropriate for toxicity testing. Cadmium (Cd) is a heavy metal with known toxic effects on several organisms, which include endocrine disruption and activation of the cellular stress responses. There is scarce genomic information on P. acuta; hence, in this work, we identify several genes related to the hormonal system, the stress response and the detoxification system to evaluate the effects of Cd. The transcriptional activity of the endocrine-related genes oestrogen receptor (ER), oestrogen-related receptor (ERR), and retinoid X receptor (RXR), the heat shock proteins genes hsp70 and hsp90 and a metallothionein (MT) gene was analysed in P...
January 2017: Environmental Pollution
https://www.readbyqxmd.com/read/27865806/ikaros-exploiting-and-targeting-the-hematopoietic-stem-cell-niche-in%C3%A2-b-progenitor-acute-lymphoblastic-leukemia
#15
REVIEW
Michelle L Churchman, Charles G Mullighan
Genetic alterations of IKZF1 encoding the lymphoid transcription factor IKAROS are a hallmark of high-risk B-progenitor acute lymphoblastic leukemia (ALL), such as BCR-ABL1-positive (Ph+) and Ph-like ALL, and are associated with poor outcome even in the era of contemporary chemotherapy incorporating tyrosine kinase inhibitors. Recent experimental mouse modeling of B-progenitor ALL has shown that IKZF1 alterations have multiple effects, including arresting differentiation, skewing lineage of leukemia from myeloid to lymphoid, and, in Ph+ leukemia, conferring resistance to tyrosine kinase inhibitor (TKI) therapy without abrogating ABL1 inhibition...
February 2017: Experimental Hematology
https://www.readbyqxmd.com/read/27852823/phosphorylation-of-human-retinoid-x-receptor-%C3%AE-at-serine-260-impairs-its-subcellular-localization-receptor-interaction-nuclear-mobility-and-1%C3%AE-25dihydroxyvitamin-d3-dependent-dna-binding-in-ras-transformed-keratinocytes
#16
Sylvester Jusu, John F Presley, Richard Kremer
Human retinoid X receptor alpha (hRXRα) plays a critical role in DNA binding and transcriptional activity through heterodimeric association with several members of the nuclear receptor superfamily including the human vitamin D receptor (hVDR). We previously showed that hRXRα phosphorylation at serine 260 through the Ras-Raf-Mitogen activated protein kinase extra-cellular signal regulated kinases 1 and 2 (MAP kinase ERK1/2) activation is responsible for resistance to the growth inhibitory effects of 1α, 25dihydroxyvitamin D3 (1α,25(OH)2D3), the biologically active metabolite of vitamin D3 To further investigate the mechanism of this resistance we studied intranuclear dynamics of hVDR and hRXRα tagged constructs in living cells together with endogenous and tagged protein in fixed cells...
November 16, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27849367/fetal-exposure-to-low-levels-of-the-plasticizer-dehp-predisposes-the-adult-male-adrenal-gland-for-endocrine-disruption
#17
S Lee, D B Martinez-Arguelles, E Campioli, V Papadopoulos
In utero exposure to endocrine disrupting chemicals (EDCs) may affect adult health. Di-(2-ethylhexyl) phthalate (DEHP) is an EDC widely used in the production of polyvinyl chloride products and an ubiquitous environmental contaminant. Previously, we used a rat model system to show that fetal exposure to DEHP decreased levels of major steroid hormones in adulthood and that environmentally-relevant levels of DEHP affected both gene expression and epigenomic loci that were affected by exposure to high levels. In the adrenal gland, we reported that the peroxisome proliferator-activated receptor (PPAR) and cholesterol biosynthesis pathways were sensitive targets of DEHP...
November 16, 2016: Endocrinology
https://www.readbyqxmd.com/read/27842487/molecular-interactions-of-bexarotene-a-retinoid-drug-and-alzheimer-s-a%C3%AE-peptide-a-docking-study
#18
Zeenat Mirza, Mohd Amin Beg
Alzheimer's disease (AD) pathogenesis is primarily hallmarked by the production and accumulation of amyloid beta (Aβ) peptide. Along with the understanding of the neurodegenerative disease progression and its pathophysiological mechanisms, development of anti-Aβ targeted effective therapeutics is essential for AD management. Numerous therapeutic approaches targeting the production, toxicity and removal of Aβ are being attempted worldwide. Prime need is to design inhibitors which can slow down the Aβ aggregation process in a physiological environment...
November 14, 2016: Current Alzheimer Research
https://www.readbyqxmd.com/read/27833522/histamine-h3-receptors-and-its-antagonism-as-a-novel-mechanism-for-antipsychotic-effect-a-current-preclinical-clinical-perspective
#19
REVIEW
Danish Mahmood
Histamine H3 receptors are present as autoreceptors on histaminergic neurons and as heteroreceptors on nonhistaminergic neurones. They control the release and synthesis of histamine and several other key neurotransmitters in the brain. H3 antagonism may be a novel approach to develop a new class of antipsychotic medications given the gathering evidence reporting therapeutic efficacy in several central nervous system disorders. Several medications such as cariprazine, lurasidone, LY214002, bexarotene, rasagiline, raloxifene, BL-1020 and ITI-070 are being developed to treat the negative symptoms and cognitive impairments of schizophrenia...
October 2016: International Journal of Health Sciences
https://www.readbyqxmd.com/read/27824486/novel-epigenetic-biomarkers-mediating-bisphenol-a-exposure-and-metabolic-phenotypes-in-female-mice
#20
Olivia S Anderson, Jung H Kim, Karen E Peterson, Brisa N Sanchez, Karilyn E Sant, Maureen A Sartor, Caren Weinhouse, Dana C Dolinoy
There is compelling evidence that epigenetic modifications link developmental environmental insults to adult disease susceptibility. Animal studies have associated perinatal bisphenol A (BPA) exposure to altered DNA methylation, but these studies are often limited to candidate gene and global non-loci specific approaches. Utilizing an epigenome-wide discovery platform, we elucidate epigenetic alterations in liver tissue from adult offspring (10 months) following perinatal BPA exposure at human physiologically relevant doses (50 ng, 50 μg, and 50 mg BPA/kg diet)...
November 8, 2016: Endocrinology
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