scholarly journals Carborane-based design of a potent vitamin D receptor agonist

2016 ◽  
Vol 7 (2) ◽  
pp. 1033-1037 ◽  
Author(s):  
Rocio Otero ◽  
Samuel Seoane ◽  
Rita Sigüeiro ◽  
Anna Y. Belorusova ◽  
Miguel A. Maestro ◽  
...  
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Receptor Agonist ◽  
Side Chain ◽  
Vitamin D Analog ◽  
Dihydrogen Bonding

The development of a promising clinical antitumor vitamin D analog possessing a side-chain o-carborane cluster that efficiently binds to VDR by unconventional dihydrogen bonding (BH⋯HN) is described.

scholarly journals Corepressor Excess Shifts the Two-Side Chain Vitamin D Analog Gemini from an Agonist to an Inverse Agonist of the Vitamin D Receptor

2003 ◽  
Vol 17 (10) ◽  
pp. 2028-2038 ◽  
Author(s):  
Manuel Macias Gonzalez ◽  
Petra Samenfeld ◽  
Mikael Peräkylä ◽  
Carsten Carlberg
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Inverse Agonist ◽  
Side Chain ◽  
Vitamin D Analog

A novel vitamin D analog with two double bonds in its side chain

1996 ◽  
Vol 51 (7) ◽  
pp. 887-892 ◽  
Author(s):  
Anitta Mahonen ◽  
Tiina Jääskeläinen ◽  
Pekka H. Mäenpää
Keyword(s):  
Vitamin D ◽  
Side Chain ◽  
Double Bonds ◽  
Vitamin D Analog

scholarly journals The selective vitamin D receptor agonist, elocalcitol, reduces endometriosis development in a mouse model by inhibiting peritoneal inflammation

2012 ◽  
Vol 27 (7) ◽  
pp. 2010-2019 ◽  
Author(s):  
M. Mariani ◽  
P. Vigano ◽  
D. Gentilini ◽  
B. Camisa ◽  
E. Caporizzo ◽  
...  
Keyword(s):  
Vitamin D ◽  
Mouse Model ◽  
Vitamin D Receptor ◽  
Receptor Agonist ◽  
Peritoneal Inflammation

scholarly journals The Vitamin D Analog ED-71 Is a Potent Regulator of Intestinal Phosphate Absorption and NaPi-IIb

Endocrinology ◽  
2012 ◽  
Vol 153 (11) ◽  
pp. 5150-5156 ◽  
Author(s):  
Alex J. Brown ◽  
Fanjie Zhang ◽  
Cynthia S. Ritter
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Mineral Metabolism ◽  
Oral Treatment ◽  
Fold Increase ◽  
Alveolar Type ◽  
Mrna Levels ◽  
Potent Inducer ◽  
Vitamin D Analog ◽  
Fold Induction

Abstract The vitamin D analog ED-71 [1α,25-dihydroxy-2β-(3-hydroxypropyloxy)vitamin D3] has been approved for treatment of osteoporosis in Japan, but its effects on mineral metabolism have not been fully explored. We investigated the actions of ED-71 on phosphate (Pi) absorption and induction of the intestinal sodium/phosphate cotransporters. Oral treatment of vitamin D-deficient rats with ED-71 (20 pmol every other day for 8 d) produced a maximal 8-fold increase in duodenal Pi absorption, measured by the in situ loop method, whereas 1,25-dihyroxyvitamin D3 [1,25(OH)2D3], at doses up to 150 pmol, had no effect. This action of ED-71 was attributable to a dramatic 24-fold induction of sodium-dependent Pi transporter type IIb (NaPi-IIb) mRNA in the duodenum; Pit-1 and Pit-2 mRNA levels were not increased. In vitamin D-replete rats, ED-71 treatment (50 pmol) at 72 and 24 h before death increased NaPi-IIb mRNA in the duodenum and jejunum, but not the ileum, whereas 1,25(OH)2D3 at 1000 pmol was ineffective in all segments. Single oral doses of ED-71 increased mouse intestinal NaPi-IIb mRNA and protein between 6 and 24 h. Surprisingly, rat lung NaPi-IIb was not increased by ED-71, despite its coexpression with the vitamin D receptor in alveolar type II cells. However, ED-71 did not induce intestinal NaPi-IIb in vitamin D receptor-ablated mice. The greater potency of ED-71 than 1,25(OH)2D3 on NaPi-IIb appears to be due to much higher and more prolonged levels of ED-71 in the circulation. In summary, ED-71, due to its disparate pharmacokinetics, is a much more potent inducer of intestinal Pi absorption and NaPi-IIb than 1,25(OH)2D3, suggesting a role for this analog in the treatment of Pi-wasting disorders.

scholarly journals The Therapeutic Effect of Active Vitamin D Supplementation in Preventing the Progression of Diabetic Nephropathy in a Diabetic Mouse Model

2020 ◽  
Vol 2020 ◽  
pp. 1-10
Author(s):  
Nakhoul Nakhoul ◽  
Tina Thawko ◽  
Evgeny Farber ◽  
Inbal Dahan ◽  
Hagar Tadmor ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Vitamin D ◽  
Diabetic Nephropathy ◽  
Vitamin D Receptor ◽  
Receptor Activation ◽  
Receptor Expression ◽  
Active Vitamin ◽  
Active Vitamin D ◽  
Vitamin D Analog

Background. Diabetic nephropathy (DN) is one of the most common microvascular complications of diabetes and is the leading cause of end-stage renal disease (ESRD) and replacement therapy worldwide. Vitamin D levels in DN patients are very low due to the decrease in the synthesis and activity of 1-α hydroxylase in the proximal tubule cells and decrease in the vitamin D receptor abundance. To date, few studies have shown the antioxidant effects of 1α,25-dihydroxyvitamin D3 [1,25(OH)2D3] on hyperglycemia-induced renal injury. The selective activator of the vitamin D receptor, paricalcitol, reduces proteinuria and slows the progression of kidney injury. The precise mechanism through which vitamin D affects diabetic status and provides kidney protection remains to be determined. Methods. Diabetes mellitus (DM) was induced in 94 8-week-old DBA/2J mice by intraperitoneal injection of streptozotocin (STZ). DM mice were randomly divided into receiving vehicle or treatment with paricalcitol, the active vitamin D analog, 1 week after DM induction or paricalcitol treatment 3 weeks after DM induction. An additional control group of healthy wild-type mice was not treated. Urine albumin, blood urea nitrogen, and creatinine levels were measured before and at the end of the paricalcitol treatment. Periodic acid-Schiff, immunohistochemistry staining, and western blot of the renal tissues of vitamin D receptor, villin, nephrin, and podocin expressions, were analyzed. Results. Paricalcitol treatment restored villin, nephrin, and podocin protein levels that were downregulated upon DM induction, and reduced fibronectin protein level. Vitamin D receptor activation by paricalcitol may reduce proteinuria of DN in mice and alleviate high-glucose-induced injury of kidney podocytes by regulating the key molecules such nephrin-podocin. Conclusions. Paricalcitol treatment was associated with improved structural changes in type 1 diabetic mice including upregulation of vitamin D receptor expression, and decreased fibrosis markers such as fibronectin. These effects may contribute to the consistent benefit of vitamin D analog to slow the deterioration in glomerular function and reduce the risk of ESRD in patients with type 1 and 2 diabetes mellitus. Our results suggest that additional use of paricalcitol may be beneficial in treating patients with diabetes under standard therapeutic strategies.

The vitamin D receptor as a target for the treatment of breast cancer: Studies with the low calcemic vitamin D analog, inecalcitol.

2016 ◽  
Vol 34 (15_suppl) ◽  
pp. e12011-e12011
Author(s):  
Alyson M. Murray ◽  
Stephen F. Madden ◽  
Naoise C Synnott ◽  
John Crown ◽  
Norma O'Donovan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Vitamin D ◽  
Vitamin D Receptor ◽  
Vitamin D Analog ◽  
Cancer Studies

The First Locked Side-Chain Analogues of Calcitriol (1α,25-Dihydroxyvitamin D3) Induce Vitamin D Receptor Transcriptional Activity

2003 ◽  
Vol 5 (22) ◽  
pp. 4033-4036 ◽  
Author(s):  
Xenxo Pérez-García ◽  
Antonio Rumbo ◽  
María Jesús Larriba ◽  
Paloma Ordóñez ◽  
Alberto Muñoz ◽  
...  
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Transcriptional Activity ◽  
Side Chain ◽  
Dihydroxyvitamin D3
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