Vitamin D and its synthetic analogs

MA Maestro, F Molnar, C Carlberg - Journal of medicinal chemistry, 2019 - ACS Publications
For many individuals, in particular during winter, supplementation with the secosteroid
vitamin D3 is essential for the prevention of bone disorders, muscle weakness, autoimmune …

Strategies for develo** pregnane X receptor antagonists: Implications from metabolism to cancer

SC Chai, WC Wright, T Chen - Medicinal research reviews, 2020 - Wiley Online Library
Pregnane X receptor (PXR) is a ligand‐activated nuclear receptor (NR) that was originally
identified as a master regulator of xenobiotic detoxification. It regulates the expression of …

Multidomain architecture of estrogen receptor reveals interfacial cross-talk between its DNA-binding and ligand-binding domains

W Huang, Y Peng, J Kiselar, X Zhao… - Nature …, 2018 - nature.com
Human estrogen receptor alpha (hERα) is a hormone-responsive nuclear receptor (NR)
involved in cell growth and survival that contains both a DNA-binding domain (DBD) and a …

Chemical protein degradation approach and its application to epigenetic targets

Y Itoh - The Chemical Record, 2018 - Wiley Online Library
In addition to traditional drugs, such as enzyme inhibitors, receptor agonists/antagonists,
and protein‐protein interaction inhibitors as well as genetic technology, such as RNA …

An alternative conformation of ERβ bound to estradiol reveals H12 in a stable antagonist position

PCT Souza, LC Textor, DC Melo, AS Nascimento… - Scientific reports, 2017 - nature.com
The natural ligand 17β-estradiol (E2) is so far believed to induce a unique agonist-bound
active conformation in the ligand binding domain (LBD) of the estrogen receptors (ERs) …

A multidisciplinary approach disclosing unexplored Aflatoxin B1 roles in severe impairment of vitamin D mechanisms of action

M Persico, R Sessa, E Cesaro, I Dini… - Cell Biology and …, 2023 - Springer
Abstract Aflatoxin B1 (AFB1), produced by fungi of the genus Aspergillus, is the most toxic
and carcinogenic mycotoxin among the classes of aflatoxins. Previous research showed that …

Identification of the histidine residue in vitamin D receptor that covalently binds to electrophilic ligands

M Yoshizawa, T Itoh, T Hori, A Kato… - Journal of Medicinal …, 2018 - ACS Publications
We designed and synthesized vitamin D analogues with an electrophile as covalent
modifiers for the vitamin D receptor (VDR). Novel vitamin D analogues 1–4 have an …

[HTML][HTML] Cyclization reaction-based turn-on probe for covalent labeling of target proteins

H Kojima, Y Fujita, R Takeuchi, Y Ikebe, N Ohashi… - Cell Chemical …, 2020 - cell.com
Fluorescent molecules have contributed to basic biological research but there are currently
only a limited number of probes available for the detection of non-enzymatic proteins. Here …

Integral approach to biomacromolecular structure by analytical-ultracentrifugation and small-angle scattering

K Morishima, A Okuda, R Inoue, N Sato… - Communications …, 2020 - nature.com
Currently, a sample for small-angle scattering (SAS) is usually highly purified and looks
monodispersed: The Guinier plot of its SAS intensity shows a fine straight line. However, it …

Alternative binding sites at the vitamin D receptor and their ligands

TR Mutchie, BY Olivia, ES Di Milo, LA Arnold - Molecular and cellular …, 2019 - Elsevier
In recent decades, the majority of ligands developed for the vitamin D receptor (VDR) bind at
its deeply buried genomic ligand binding pocket. Theses ligands can be categorized into …