Marina Grimaldi
YOU?
Author Swipe
View article: Human and zebrafish mineralocorticoid receptors reporter cell assays to assess the activity of chemicals
Human and zebrafish mineralocorticoid receptors reporter cell assays to assess the activity of chemicals Open
The action of environmental chemicals (ECs) on the mineralocorticoid receptor (MR) has been suggested to impair physiological processes regulated by this nuclear receptor. However, it remains understudied both as a target of ECs and with r…
View article: Distinct 2-phenyl-imidazo[1, 2α] pyridine derivatives drive ER degradation and selectively impair proliferation of ER<sup>+</sup> breast cancer cells via the aryl hydrocarbon receptor
Distinct 2-phenyl-imidazo[1, 2α] pyridine derivatives drive ER degradation and selectively impair proliferation of ER<sup>+</sup> breast cancer cells via the aryl hydrocarbon receptor Open
X15695 is a 2-phenyl-imidazo[1, 2α] pyridine derivative identified as an orally active, selective oestrogen receptor (ER) degrader that inhibits the proliferation of ER + breast cancer cells. Here, we show that X15695 is an aryl hydrocarbo…
View article: Inter-laboratory validation study of an in vitro glucocorticoid receptor transactivation assay for testing potential endocrine disrupting chemicals
Inter-laboratory validation study of an in vitro glucocorticoid receptor transactivation assay for testing potential endocrine disrupting chemicals Open
The glucocorticoid receptor (GR) belongs to the family of steroid receptors (SRs). These receptors regulate a vast selection of cell-, tissue-, and organism biology, and are also targets of endocrine disrupting chemicals warranting design …
View article: An abundant ginger compound furanodienone alleviates gut inflammation via the xenobiotic nuclear receptor PXR in mice
An abundant ginger compound furanodienone alleviates gut inflammation via the xenobiotic nuclear receptor PXR in mice Open
The literature documenting the value of drug-like molecules found in natural products is vast. Although many dietary and herbal remedies have been found to be effective for treating intestinal inflammation, the identification of their acti…
View article: Toward the Manufacturing of a Non-Toxic High-Performance Biobased Epoxy–Hemp Fibre Composite
Toward the Manufacturing of a Non-Toxic High-Performance Biobased Epoxy–Hemp Fibre Composite Open
This study describes the production of a new biobased epoxy thermoset and its use with long hemp fibres to produce high-performance composites that are totally biobased. The synthesis of BioIgenox, an epoxy resin derived from a lignin bior…
View article: WITHDRAWN: Proton transfer from bisphenol-A is required to activate extranuclear-initiated estrogen receptor signaling
WITHDRAWN: Proton transfer from bisphenol-A is required to activate extranuclear-initiated estrogen receptor signaling Open
Withdrawal Statement The authors have withdrawn this manuscript because they have identified errors in the western blots in Figures 1B, C, and G, as well as in Figure 2 A and B. Therefore, the authors do not wish this work to be cited as r…
View article: Structural Insights into the Activation of Human Aryl Hydrocarbon Receptor by the Environmental Contaminant Benzo[a]pyrene and Structurally Related Compounds
Structural Insights into the Activation of Human Aryl Hydrocarbon Receptor by the Environmental Contaminant Benzo[a]pyrene and Structurally Related Compounds Open
The aryl hydrocarbon receptor (AHR) is a ligand-dependent transcription factor belonging to the bHLH/PAS protein family and responding to hundreds of natural and chemical substances. It is primarily involved in the defense against chemical…
View article: Steatosis and Metabolic Disorders Associated with Synergistic Activation of the CAR/RXR Heterodimer by Pesticides
Steatosis and Metabolic Disorders Associated with Synergistic Activation of the CAR/RXR Heterodimer by Pesticides Open
The nuclear receptor, constitutive androstane receptor (CAR), which forms a heterodimer with the retinoid X receptor (RXR), was initially reported as a transcription factor that regulates hepatic genes involved in detoxication and energy m…
View article: 2,4-Di-tert-butylphenol Induces Adipogenesis in Human Mesenchymal Stem Cells by Activating Retinoid X Receptors
2,4-Di-tert-butylphenol Induces Adipogenesis in Human Mesenchymal Stem Cells by Activating Retinoid X Receptors Open
2,4-Di-tert-butylphenol (2,4-DTBP) is an important commercial antioxidant and a toxic natural secondary metabolite that has been detected in humans. However, there is scant information regarding its toxicological effects. We asked whether …
View article: Understanding glycidylation reaction for the formation of pure mono, diglycidyl and dual monomers as glycidyl methacrylate of vanillyl alcohol
Understanding glycidylation reaction for the formation of pure mono, diglycidyl and dual monomers as glycidyl methacrylate of vanillyl alcohol Open
The mono epoxy methacrylate and the diepoxy of vanillyl alcohol (DGEVA) are products already known and reported in literature. However, their respective synthesis processes lead to mixtures of products and side‐products. Hence, the final r…
View article: Straightforward sustainable synthesis of novel non-endocrine disruptive bio-based organic UV-B filters with antimicrobial activity
Straightforward sustainable synthesis of novel non-endocrine disruptive bio-based organic UV-B filters with antimicrobial activity Open
With an increasing demand for safe and natural products from both industries and consumers, paired with the recent ban of decried molecules (i.e. octinoxate, avobenzone or octocrylene) due to their high negative impact on humans and the en…
View article: 2,4-Di-tert-butylphenol Induces Adipogenesis in Human Mesenchymal Stem Cells by Activating Retinoid X Receptors
2,4-Di-tert-butylphenol Induces Adipogenesis in Human Mesenchymal Stem Cells by Activating Retinoid X Receptors Open
2,4-di-tert-butylphenol (2,4-DTBP) is an important commercial antioxidant and a toxic natural secondary metabolite that has been detected in humans. However, there is scant information regarding its toxicological effects. Here we asked whe…
View article: Cryo-EM structure of the agonist-bound Hsp90-XAP2-AHR cytosolic complex
Cryo-EM structure of the agonist-bound Hsp90-XAP2-AHR cytosolic complex Open
Summary Living organisms have developed protein sensors helping them to adapt to their environment 1 . The aryl hydrocarbon receptor (AHR) is an emblematic member of this class of proteins, and a ligand-dependent transcription factor that …
View article: Structure-Based and Knowledge-Informed Design of B-Raf Inhibitors Devoid of Deleterious PXR Binding
Structure-Based and Knowledge-Informed Design of B-Raf Inhibitors Devoid of Deleterious PXR Binding Open
Dabrafenib is an anticancer drug currently used in the clinics, alone or in combination. However, dabrafenib was recently shown to potently activate the human nuclear receptor pregnane X receptor (PXR). PXR activation increases the clearan…
View article: A Comparative Study of Human and Zebrafish Pregnane X Receptor Activities of Pesticides and Steroids Using In Vitro Reporter Gene Assays
A Comparative Study of Human and Zebrafish Pregnane X Receptor Activities of Pesticides and Steroids Using In Vitro Reporter Gene Assays Open
The nuclear receptor pregnane X receptor (PXR) is a ligand-dependent transcription factor that regulates genes involved in xenobiotic metabolism in mammals. Many studies suggest that PXR may play a similar role in fish. The interaction of …
View article: Mechanistic insights into the synergistic activation of the RXR–PXR heterodimer by endocrine disruptor mixtures
Mechanistic insights into the synergistic activation of the RXR–PXR heterodimer by endocrine disruptor mixtures Open
Significance Many environmental pollutants act as endocrine disruptors that interfere with normal endocrine regulation and promote adverse effects in humans. As a major target of xenobiotics, the pregnane X receptor (PXR) is known to play …
View article: A Novel N-Substituted Valine Derivative with Unique Peroxisome Proliferator-Activated Receptor γ Binding Properties and Biological Activities
A Novel N-Substituted Valine Derivative with Unique Peroxisome Proliferator-Activated Receptor γ Binding Properties and Biological Activities Open
A proprietary library of novel N-aryl-substituted amino acid derivatives bearing a hydroxamate head group allowed the identification of compound 3a that possesses weak proadipogenic and peroxisome proliferator-activated receptor γ (PPARγ) …
View article: Assessing the Selectivity of FXR, LXRs, CAR, and RORγ Pharmaceutical Ligands With Reporter Cell Lines
Assessing the Selectivity of FXR, LXRs, CAR, and RORγ Pharmaceutical Ligands With Reporter Cell Lines Open
To characterize human nuclear receptor (NR) specificity of synthetic pharmaceutical chemicals we established stable cell lines expressing the ligand binding domains (LBDs) of human FXR, LXRα, LXRβ, CAR, and RORγ fused to the yeast GAL4 DNA…
View article: The Anti-Cancer Drug Dabrafenib Is a Potent Activator of the Human Pregnane X Receptor
The Anti-Cancer Drug Dabrafenib Is a Potent Activator of the Human Pregnane X Receptor Open
The human pregnane X receptor (hPXR) is activated by a large set of endogenous and exogenous compounds and plays a critical role in the control of detoxifying enzymes and transporters regulating liver and gastrointestinal drug metabolism a…
View article: High Content Screening Using New U2OS Reporter Cell Models Identifies Harmol Hydrochloride as a Selective and Competitive Antagonist of the Androgen Receptor
High Content Screening Using New U2OS Reporter Cell Models Identifies Harmol Hydrochloride as a Selective and Competitive Antagonist of the Androgen Receptor Open
Prostate cancer is the most commonly diagnosed malignancy in men. Its growth mainly relies on the activity of the androgen receptor (AR), justifying the use of androgen deprivation therapy as a gold standard treatment for the metastatic di…