[HTML][HTML] Vitamin D and its receptor from a structural perspective

N Rochel - Nutrients, 2022 - mdpi.com
The activities of 1α, 25-dihydroxyvitamin D3, 1, 25D3, are mediated via its binding to the
vitamin D receptor (VDR), a ligand-dependent transcription factor that belongs to the nuclear …

Further Studies on the Highly Active Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D3 (Calcitriol): Refinement of the Side Chain

A Zárate-Ruíz, S Seoane, C Peluso-Iltis… - Journal of Medicinal …, 2023 - ACS Publications
Current efforts in the vitamin D field are directed toward the development of highly
antiproliferative yet noncalcemic analogues of the natural hormone 1α, 25-dihydroxyvitamin …

Design, Synthesis, Biological Activity, and Structural Analysis of Novel Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D3

S Seoane, P Gogoi, A Zárate-Ruíz… - Journal of Medicinal …, 2022 - ACS Publications
The toxic calcemic effects of the natural hormone 1α, 25-dihydroxyvitamin D3 (1, 25D3, 1, 25-
dihydroxycholecalciferol) in the treatment of hyperproliferative diseases demand the …

[HTML][HTML] Cytosolic sequestration of the vitamin D receptor as a therapeutic option for vitamin D-induced hypercalcemia

D Rovito, AY Belorusova, S Chalhoub, AI Rerra… - Nature …, 2020 - nature.com
The bioactive vitamin D3, 1α, 25 (OH) 2D3, plays a central role in calcium homeostasis by
controlling the activity of the vitamin D receptor (VDR) in various tissues. Hypercalcemia …

[HTML][HTML] Syntheses of 25-Adamantyl-25-alkyl-2-methylidene-1α,25-dihydroxyvitamin D3 Derivatives with Structure–Function Studies of Antagonistic and Agonistic …

K Maekawa, M Ishizawa, T Ikawa, H Sajiki… - Biomolecules, 2023 - mdpi.com
The active form of vitamin D3, 1α, 25-dihydroxyvitamin D3 [1, 25 (OH) 2D3], is a major
regulator of calcium homeostasis through activation of the vitamin D receptor (VDR). We …

Molecular determinants of MED1 interaction with the DNA bound VDR–RXR heterodimer

AY Belorusova, M Bourguet, S Hessmann… - Nucleic acids …, 2020 - academic.oup.com
The MED1 subunit of the Mediator complex is an essential coactivator of nuclear receptor-
mediated transcriptional activation. While structural requirements for ligand-dependent …

Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors In Vivo

N Khazan, KK Kim, JN Hansen, NA Singh… - Journal of medicinal …, 2022 - ACS Publications
Vitamin-D receptor (VDR) mRNA is overexpressed in neuroblastoma and carcinomas of
lung, pancreas, and ovaries and predicts poor prognoses. VDR antagonists may be able to …

Oligoarginine-conjugated peptide foldamers inhibiting vitamin D receptor-mediated transcription

M Takyo, Y Sato, N Hirata, K Tsuchiya, H Ishida… - ACS …, 2022 - ACS Publications
The vitamin D receptor (VDR) is a nuclear receptor, which is involved in several
physiological processes, including differentiation and bone homeostasis. The VDR is a …

Chronic exposure to tralopyril induced abnormal growth and calcium regulation of turbot (Scophthalmus maximus)

B Liu, P Li, S He, S Xing, C Chen, L Liu, ZH Li - Chemosphere, 2022 - Elsevier
Tralopyril is an emerging marine antifouling agent with limited data on its effects on fish
growth and calcium regulation. To determine the changes induced by long-term exposure to …

Design, synthesis and evaluation of side-chain hydroxylated derivatives of lithocholic acid as potent agonists of the vitamin D receptor (VDR)

CM González, S Gaikwad, G Lasanta, J Loureiro… - Bioorganic …, 2021 - Elsevier
A high number of biologically active and low-calcemic secosteroidal ligands of the vitamin D
receptor (VDR) have been developed, some of which are already used clinically although …