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Receptors, Calcitriol (0):
Recent article
Receptors, Calcitriol
Abstract
We found that bb genotype of BsmI polymorphism conferred significant risk to smear positive and multiple drug resistant (MDR) TB in tribes [OR (CI)=3.7 (1.5-9.2), p=0.002], SE population [OR (CI)=2.1 (1.4-3.3), p=0.0004] and Muslims [OR (CI)=6.7 (1.1-39), p=0.01]. The subjects with FF genotype of Fo...
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PMID: 21645645
PDF is available here.
PDF is available here.
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Abstract
Nuclear receptors (NRs) are ligand-activated transcription factors that are important to life by regulating a wide variety of physiological and pathological functions. There are three classes of NRs defined by ligands and heterodimer partners. The Class II NRs are involved in a broad...
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PMID: 21554208
PDF is available here.
PDF is available here.
Discovery medicine (11)59 2011
Abstract
We place emphasis on the regulatory roles of vitamin D(3) on autophagy at different steps, including induction, nucleation, elongation to maturation, and degradation. We summarize the known molecular mechanisms of vitamin D/VDR signaling on autophagy homeostasis. The potential application of the ins...
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PMID: 21524386
PDF is available here.
PDF is available here.
British Journal of Nutrition (105)1 2011
Abstract
Inter-individual response differences to vitamin D and Ca supplementation may be under genetic control through vitamin D and oestrogen receptor genes, which may influence their absorption and/or metabolism. Metabolomic studies on blood and urine from subjects supplemented with Ca and vitamin D revea...
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PMID: 20727239
PDF is available here.
PDF is available here.
British Journal of Nutrition (105)2 2011
Abstract
I collagen and osteocalcin mRNA and the ratio of osteoprotegerin/receptor activator of NF-κB ligand mRNA, and suppressed the increase in IL-6 mRNA induced by OVX in the femur of mice. The present results indicate that the optimal dosage of the TF fraction of HEP for the improvement of bone properti...
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PMID: 20815976
PDF is available here.
PDF is available here.
Abstract
Significant advances have been made in the characterization of Vitamin D and the Vitamin D receptor (VDR) in immune function. The studies of signaling pathways involved in the response to infection and inflammation have led to a more detailed understanding of the cellular response to Vitamin D throu...
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PMID: 20639756
PDF is available here.
PDF is available here.
Abstract
We examine whether calcitriol increases chemotherapy or tyrosine kinase inhibitor in vitro cytotoxicity in canine mastocytoma C2 cells. We also evaluate the in vivo effect of DN101, a highly concentrated oral formulation of calcitriol designed specifically for cancer therapy, as a single-agent thera...
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PMID: 20691028
PDF is available here.
PDF is available here.
Behavioural Pharmacology (21)5-6 2010
Abstract
We discuss mounting evidence, and parallel recent clinical and animal behavioral, genetic and pharmacological data to emphasize the emerging role of the neurosteroid vitamin D system in brain function....
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PMID: 20571365
PDF is available here.
PDF is available here.
Abstract
We have identified 14 common and clinically relevant conditions of contemporary nature that are related to the kidney bone disease, including calcitriol (active vitamin D) deficiency, 25(OH)-vitamin D deficiency, biochemical hyperparathyroidism, relatively low parathyroid hormone (PTH) level, increa...
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PMID: 20671739
PDF is available here.
PDF is available here.
Abstract
We examined two unrelated young female patients who exhibited severe early onset rickets, hypocalcemia, and hypophosphatemia. Both patients had partial alopecia but with different unusual patterns of scant hair. Sequencing of the VDR gene showed that both patients harbored the same unique nonsense m...
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PMID: 21073129
PDF is available here.
PDF is available here.
Abstract
We have prospectively assessed the influence of GHR and VDR gene polymorphisms on the response to rhGH therapy in Venezuelan children with growth hormone deficiency (GHD, n=28) and Turner syndrome (TS, n=25). Clinical data during rhGH treatment were compared in GH and TS patients with different geno...
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PMID: 21073120
PDF is available here.
PDF is available here.
Abstract
Vitamin D and the vitamin D receptor (VDR) have been shown to be important regulators of the immune system. In particular, vitamin D and VDR deficiency exacerbates experimental autoimmune diseases such as inflammatory bowel disease (IBD). IBD develops due to an immune-mediated attack by pathogenic T-...
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PMID: 20515520
PDF is available here.
PDF is available here.
Abstract
We will spotlight the molecular mechanisms of receptor/ligand function and how bile acid-activated receptors regulate the innate immunity in the gastrointestinal tract and liver. The ability of these receptors to integrate metabolic and inflammatory signaling makes them particularly attractive targe...
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PMID: 20642438
PDF is available here.
PDF is available here.
Experimental Hematology (38)8 2010
Abstract
We previously showed that Gemini-23-yne-26,27-hexafluoro-D(3) inhibited the proliferation of MCF-7 breast cancer cells in association with inhibition of the mammalian target of rapamycin (mTOR) signaling. This study explored the drug interaction of 1,25(OH)(2)D(3) and rapamycin analog RAD001 (everol...
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PMID: 20382200
PDF is available here.
PDF is available here.
Abstract
1,25D3 potentiates gemcitabine and cisplatin-mediated growth inhibition in human bladder cancer models in vitro and in vivo, which involves p73 induction and apoptosis....
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PMID: 20564622
PDF is available here.
PDF is available here.
Urologia Internationalis (85)1 2010
Abstract
We chose 50 Chinese subjects with normal urinary citrate levels (N) and 31 Chinese subjects with idiopathic hypocitraturia (L). The VDR polymorphisms BsmI, FokI, TaqI, and ApaI were detected using the PCR-RFLP technique, and the relationship between these polymorphisms and the presence of idiopathic...
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PMID: 20339297
PDF is available here.
PDF is available here.
Clinical Immunology (136)1 2010
Abstract
Our aim was to verify whether the vitamin D analogue ZK 156979 (ZK) down-regulates adhesion molecules, and decreases MMPs production by PBMC of IBD patients. ICAM-1 and LFA-1 levels increase, when PBMC were incubated with PHA or LPS or TNF-alpha, and decrease when these substances were used in combi...
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PMID: 20399147
PDF is available here.
PDF is available here.
Abstract
There is a correlation between vitamin D receptor genetic polymorphism Fok I and vitamin D deficiency rickets. This suggests that vitamin D receptor genetic polymorphism might play an important role in determining susceptibility to development of vitamin D deficiency rickets....
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PMID: 20637153
PDF is available here.
PDF is available here.
Cancer Biology & Therapy (10)1 2010
Abstract
The developmental Hedgehog (Hh) pathway has been shown to cause malignancies in the adult organism, specifically in the proximal gastrointestinal tract. Previous studies have used the Hh-inhibitory alkaloid cyclopamine to treat Hh-dependent tumor growth. The present study aimed to de...
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PMID: 20495364
PDF is available here.
PDF is available here.
Abstract
We previously showed that the vitamin D receptor (VDR) is subject to degradation by the 26S proteasome and that treatment with 1,25-dihydroxyvitamin D(3) (1,25D(3)) inhibited this degradation. In the present study, we found that in osteoblasts, but not in intestinal epithelial cells, the VDR was sus...
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PMID: 20564192
PDF is available here.
PDF is available here.
Clinical calcium (20)7 2010
Abstract
Disturbances in bone and mineral metabolism in patients with chronic kidney disease (CKD) affect not only the bone diseases but also other organ disorders in the whole body and deteriorate the survival of these patients. The term CKD-Mineral and Bone Disorder (CKD-MBD) has been established describin...
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PMID: 20585177
PDF is available here.
PDF is available here.
Clinical calcium (20)7 2010
Abstract
Recently, many investigators have reported that treatment with vitamin D improves outcomes of patients with chronic kidney disease. Though the detailed mechanisms have remained unclear, it has been speculated that such a treatment may prevent progression of chronic kidney disease and cardiovascular...
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PMID: 20585183
PDF is available here.
PDF is available here.
Clinical calcium (20)7 2010
Abstract
We examined both in vitro and in vivo the potential use of RNAi to suppress PTH production in PT cells of SHPT patients. These results provide the findings to understand the mechanism and new treatment to SHPT....
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PMID: 20585184
PDF is available here.
PDF is available here.
Abstract
We previously reported that 1alpha,25(OH)2D3 induces non-transcriptional rapid responses through activation of MAPKs in C2C12 skeletal muscle cells. However, there is little information on the molecular mechanism underlying the initiation of 1alpha,25(OH)2D3 signaling through this pathway. Plasma me...
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PMID: 20211253
PDF is available here.
PDF is available here.
Abstract
We recently reported that 22S-butyl-1alpha,24R-dihydroxyvitamin D(3)3 recovers the agonistic activity for vitamin D receptor (VDR), although its 25,26,27-trinor analog 2 is a potent VDR antagonist. To investigate the structural features involved in the recovery of agonism, we crystallized the ternar...
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PMID: 20211257
PDF is available here.
PDF is available here.
Abstract
We surmised that gestational vitamin D deficiency is a risk factor for MS. To test this hypothesis, a vitamin D deficiency was induced in C57BL/6 female mice 6 weeks prior to conception and prolonged until offspring birth. Contrary to our prediction, we show here that adult offspring exposed to deve...
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PMID: 20214984
PDF is available here.
PDF is available here.
Abstract
We used a single nucleotide polymorphism (SNP) tagging approach to evaluate the association between SNPs in VDR and RXRA and serum levels of 1,25(OH)2D and 25(OH)D. A total of 42 tagSNPs in VDR and 32 in RXRA were analyzed in a sample of 415 participants. Principal components analyses revealed a gen...
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PMID: 20307661
PDF is available here.
PDF is available here.
Abstract
We show that in HL60 and in THP-1 cells VDR protein interacts with heat shock protein 90 (Hsp90) and that Hsp90 is important for differentiation of AML cells. Geldanamycin (GA), an Hsp90 inhibitor, is able to suppress 1,25-induced differentiation of HL60 cells.
Copyright (c) 2010 Elsevier Ltd. All r...
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PMID: 20138989
PDF is available here.
PDF is available here.
Abstract
We have found that the transcription factors Snail1 and Snail2, known as inducers of epithelial-to-mesenchymal transition (EMT), inhibit VDR expression and block 1,25(OH)2D3 action in colon cancer cells. Snail1 and Snail2 have an additive repressing effect on VDR gene promoter. These effects are spe...
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PMID: 20138990
PDF is available here.
PDF is available here.
Abstract
2beta-substituted analogs of 14-epi-previtamin D(3) were synthesized for the first time by the thermal isomerization of the corresponding 14-epi-vitamin D3 that were available using coupling reaction between the A-ring phosphine oxide derived from a chiral epoxide and CD-ring cis-hydrindanone. The V...
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PMID: 20214990
PDF is available here.
PDF is available here.
Abstract
The nuclear vitamin D receptor (VDR) binds 1,25-dihydroxyvitamin D3 (1,25D), its high affinity renal endocrine ligand, to signal intestinal calcium and phosphate absorption plus bone remodeling, generating a mineralized skeleton free of rickets/osteomalacia with a reduced risk of osteoporotic fractu...
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PMID: 20227497
PDF is available here.
PDF is available here.
Abstract
We evaluated the energies of the interactions between the LBP residues and 1alpha,25(OH)2D3 by using an ab initio fragment molecular orbital (FMO) method at the Møller-Plesset second-order perturbation (MP2) level. This FMO-MP2 method can be used to correctly evaluate both electrostatic and van der...
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PMID: 20236613
PDF is available here.
PDF is available here.
Abstract
We have demonstrated that paricalcitol, a VDRA, ameliorates left ventricular hypertrophy (LVH) in uremic rats by up-regulating the VDR, decreasing myocardial PCNA and also decreasing myocardial oxidative stress. Thus, paricalcitol can suppress the progression of LVH, myocardial and perivascular fibr...
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PMID: 20236614
PDF is available here.
PDF is available here.
Abstract
We used an in silico computational method to theoretically analyze important residue-ligand interactions as well as ligand conformation changes in the vitamin D receptor (VDR). The ligand used for analysis was 1alpha,25-dihydroxy-19-nor-vitamin D3 [1alpha,25-19-nor-(OH)2D3] [1,2], whose crystal stru...
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PMID: 20236615
PDF is available here.
PDF is available here.
Abstract
We obtained (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (5). This analog, designated 2MD, is characterized by a significantly enhanced calcemic activity and is currently evaluated as a potential drug for osteoporosis. Therefore, it was of interest to synthesize also its 1-desoxy analog an...
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PMID: 20347975
PDF is available here.
PDF is available here.
Abstract
We have demonstrated amplified CYP24 expression in uremic rats, suggesting that CYP24 has an etiological role in vitamin D insufficiency commonly associated with chronic kidney disease (CKD). We have designed two new analogues of 1alpha,25-dihydroxyvitamin D3 (1alpha,25(OH)2D3), namely CTA091 and CT...
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PMID: 20347976
PDF is available here.
PDF is available here.
Abstract
We have compared fracture repair between Cyp24a1-/- mice and wild-type controls. We have observed a delay in the mineralization of the cartilaginous matrix of the soft callus in Cyp24a1-/- mutant animals, accompanied by reduced expression of chondrocyte marker genes. These results show that Cyp24a1...
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PMID: 20144713
PDF is available here.
PDF is available here.
Abstract
The active metabolite of vitamin D, 1,25-dihydroxyvitamin D, has been shown to have pro-differentiation and antiproliferative effects on keratinocytes that are mediated by interactions with its nuclear receptor. Other cutaneous actions of the vitamin D receptor have been brought to light by the cuta...
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PMID: 20138991
PDF is available here.
PDF is available here.
Abstract
Among more than 3000 analogs of 1alpha,25-dihydroxyvitamin D3 synthesized to date, only a few were characterized by structural modifications in the seco-B-ring. The compounds alkylated at C-6 seemed to be interesting targets for synthetic efforts. Such vitamin D analogs easily undergo thermal conver...
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PMID: 20153829
PDF is available here.
PDF is available here.
Abstract
We have cloned the cDNA for the human VDR into the pTwin1 expression system. The expression system results in the cDNA for a chitin-binding peptide and a yeast intein fused in frame with the N-terminal end of the cDNA for VDR. The intein cDNA codes for a self-cleaving peptide that can release VDR, w...
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PMID: 20171280
PDF is available here.
PDF is available here.
Abstract
We report the crystal structure of human VDR H305Q-ligand binding domain bound to 1alpha,25(OH)2D3 solved at 1.8A resolution. The protein adopts the active conformation of the wild-type liganded VDR. A local conformational flexibility at the mutation site weakens the hydrogen bond between the 25-OH...
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PMID: 20403435
PDF is available here.
PDF is available here.
Abstract
We require a thorough understanding of how common single nucleotide polymorphisms (SNPs) influence serum concentrations of 25-hydroxyvitamin D (25OHD). We undertook a systematic review of the literature in order to identify studies that examined 25OHD concentrations, and common SNPs. We found nine s...
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PMID: 20363324
PDF is available here.
PDF is available here.
Abstract
We detected expression of VDR and the vitamin D metabolising enzymes in normal kidney. VDR and CYP27B1 were strongly expressed in proximal tubules, while CYP2R1 and CYP27A1 had a marked expression in distal tubules. In CCc expression was lost for VDR and all the enzymes, except for very few cells ex...
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PMID: 20362668
PDF is available here.
PDF is available here.
Abstract
We have compared tumor progression in the LPB-Tag model of prostate in VDR knock out (VDRKO) and wild type (VDRWT) mice. On the C57BL/6 background LPB-Tag tumors progress significantly more rapidly in the VDRKO mice. VDRKO tumors show significantly higher levels of cell proliferation than VDRWT tumo...
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PMID: 20347977
PDF is available here.
PDF is available here.
Abstract
We now know that when cells of the immune system such a macrophages sense a bacterial infection they acquire the capacity to convert circulating 25D into 1,25D. Moreover, 1,25D thus produced is a direct inducer of expression of genes encoding antimicrobial peptides, in particular cathelicidin antimi...
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PMID: 20302931
PDF is available here.
PDF is available here.
Abstract
We investigated the expression and kinetics of vitamin D-related genes in human activated T lymphocytes. Different activation stimuli elicited increased VDR- and 1-alpha-hydroxylase expression, with a highly similar kinetic pattern. Addition of 1,25(OH)2D3 effectively triggered VDR signaling, as evi...
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PMID: 20302932
PDF is available here.
PDF is available here.
Abstract
We show that 1alpha,25-dihydroxyvitamin D3 (1,25(OH)2D3) and a synthetic non-genotropic vitamin D analog agonist, 1a,25(OH)2-lumisterol (JN), exhibit similar rapid effects on sarcomere shortening (contraction) of isolated adult cardiomyocyte. We also report that the vitamin D receptor (VDR) specific...
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PMID: 20304057
PDF is available here.
PDF is available here.
Abstract
We orally administered the compound at 0.03 microg/kg to a beagle model with spontaneous BPH. Prostate volume was checked by rectal ultrasonic probe periodically during 11 months of administration and the prostate tissues histologically examined. CH5036249 inhibited prostate growth in two out of thr...
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PMID: 20304062
PDF is available here.
PDF is available here.
Abstract
We have recently described the synthesis of 1alpha,25-dihydroxy-19-norvitamin D3 analogs 2 and 3, possessing an additional ring connecting their 3beta-oxygen and C-2. Such structural constrains prevent the A-ring conformational flexibility and the analogs exist exclusively in the alpha-chair form wi...
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PMID: 20214980
PDF is available here.
PDF is available here.
Abstract
We recently showed that 1,25-dihydroxyvitamin D3 and some of the investigated PPAR ligands inhibited proliferation of the human melanoma cell line MeWo. In addition to this, our results gave an indication of an interconnection of the PPAR and VDR signaling pathways at the level of cross-regulation o...
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PMID: 20214982
PDF is available here.
PDF is available here.
Abstract
We review the different classes of CD-ring analogs and highlight some representative analogs such as the fluorinated D-ring analogs CD578, WU515 and WY1113 which show markedly increased differentiating activity on human SW480-ADH colon cancer cells, characterized by a stronger induction of the invas...
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PMID: 20132886
PDF is available here.
PDF is available here.
Abstract
We found that the DRIP complex is the main complex binding to VDR in the proliferating keratinocyte, whereas SRC2 and 3 and their associated proteins are the major coactivators binding to VDR in the differentiated keratinocyte. Moreover, we have found a specific role for DRIP205 in the regulation of...
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PMID: 20298785
PDF is available here.
PDF is available here.
Abstract
We have already synthesized 1-epi-eldecalcitol, 3-epi-eldecalcitol, and 1,3-diepi-eldecalcitol with inherent biological interests of each targeted analog and evaluated their biological responses. It has been reported that 20-epi-1,25(OH)2D3, a diastereomer of 1,25(OH)2D3 that possesses an inverted m...
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PMID: 20304058
PDF is available here.
PDF is available here.
Abstract
A review of the design and synthesis of structural analogs of the vitamin D hormone recently investigated in our laboratories, and the first report on a new class of vitamin D analogs characterized by an aromatic D-ring, is described.
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
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PMID: 20346396
PDF is available here.
PDF is available here.
Abstract
We reported previously that out of seven melanoma cell lines analyzed, three cell lines (MeWo, SK-Mel28, SM) respond to the antiproliferative effects of 1,25(OH)2D3, while the others (SK-Mel5, SK-Mel25, IGR, Meljuso) are resistant. It was the aim of this study to investigate whether epigenetic mecha...
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PMID: 20153427
PDF is available here.
PDF is available here.
Abstract
We assessed genomic profiles of glandular tissue and established tumors from MMTV-neu mice fed adequate (250 IU/kg) or high (5000 IU/kg) vitamin D (cholecalciferol). Genomic profiles were also obtained in murine mammary cells that differentially express VDR that were cultured in vitro with 100 nM 1,...
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PMID: 20412854
PDF is available here.
PDF is available here.
Abstract
We developed a system for isolation of fresh endothelial cells from tumors and Matrigel environments which demonstrate that CYP24, the catabolic enzyme involved in vitamin D signaling, is epigenetically silenced selectively in tumor-derived endothelial cells (TDEC). TDEC maintain phenotypic characte...
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PMID: 20304059
PDF is available here.
PDF is available here.
Abstract
We used flexible docking in combination with whole-cell patch-clamp electrophysiology and steroid competition assays to demonstrate that (a) new non-vitamin D VDR ligands show a different pocket selectivity when compared to 1,25D3 that is qualitatively consistent with their ability to stimulate chlo...
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PMID: 20398762
PDF is available here.
PDF is available here.
Abstract
We determined the 25-hydroxycholecalciferol (25(OH2)D3) serum levels. Expression of VDR, COX-2 and 15-PGDH was determined by Western blot analysis. Serum levels of 25(OH2)D3 and PGE2 were measured by chemiluminescence-based and colorimetric immunoassay. We detected significantly higher expressions o...
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PMID: 20304053
PDF is available here.
PDF is available here.
Abstract
We discuss evidence demonstrating that in osteoblastic cells VDR binds to the nuclear matrix fraction in a 1alpha,25(OH)2D3-dependent manner. This interaction occurs rapidly after exposure to 1alpha,25(OH)2D3 and does not require a functional VDR DNA binding domain. The nuclear matrix-bound VDR mole...
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PMID: 20171279
PDF is available here.
PDF is available here.