A5073418734- Estrogen and related hormone effects
- Neuropeptides and Animal Physiology
- Neurobiology and Insect Physiology Research
- Circadian rhythm and melatonin
- Receptor Mechanisms and Signaling
- Chemical Synthesis and Analysis
- Effects and risks of endocrine disrupting chemicals
- Insect and Arachnid Ecology and Behavior
- Prion Diseases and Protein Misfolding
- Computational Drug Discovery Methods
- Bacteriophages and microbial interactions
- Chemokine receptors and signaling
- DNA and Nucleic Acid Chemistry
- Toxic Organic Pollutants Impact
- Enzyme Structure and Function
- Monoclonal and Polyclonal Antibodies Research
- Pharmacological Receptor Mechanisms and Effects
- Insect Resistance and Genetics
- Hypothalamic control of reproductive hormones
- Protein Hydrolysis and Bioactive Peptides
- Amino Acid Enzymes and Metabolism
- Glycosylation and Glycoproteins Research
- Chemistry and Chemical Engineering
- RNA and protein synthesis mechanisms
- Biochemical and Structural Characterization
Kyushu University
2014-2025
Laboratoire de Biochimie
2025
Fukuoka University
2007-2020
Istituto Superiore di Sanità
2012
Various lines of evidence have shown that bisphenol A [BPA; HO-C6H4-C(CH3)2-C6H4-OH] acts as an endocrine disruptor when present in very low doses. We recently demonstrated BPA binds strongly to human estrogen-related receptor-gamma (ERR-gamma ) a binding assay using [3H]4-hydroxytamoxifen ([3H]4-OHT). also inhibits the deactivation activity 4-OHT.In study, we intended obtain direct interacts with ERR-gamma strong binder, and clarify structural requirements for its ERR-gamma.We examined...
Many lines of evidence reveal that bisphenol A (BPA) functions at very low doses as an endocrine disruptor. The human estrogen-related receptor γ (ERRγ) behaves a constitutive activator transcription, although the endogenous ligand is unknown. We have recently demonstrated BPA binds strongly to ERRγ (KD = 5.5 nM), but not estrogen (ER). preserves ERRγ's basal activity, and protects selective ER modulator 4-hydroxytamoxifen from its deactivation ERRγ. In order shed light on molecular...
Bisphenol AF has been acknowledged to be useful for the production of CF3-containing polymers with improved chemical, thermal, and mechanical properties. Because lack adequate toxicity data, bisphenol nominated comprehensive toxicological characterization.
Estrogen-related receptor γ (ERRγ), one of the 48 human nuclear receptors, has a fully active conformation with no ligand. We recently demonstrated that ERRγ binds strongly bisphenol A (BPA), nastiest endocrine disruptors, and thus retaining ERRγ's high basal constitutive activity. report BPA accumulates in maternal–fetal placental unit led us to hypothesize large amount might exist placenta. Here we evidence placenta indeed expresses exceptionally strongly. first ascertained presence nine...
The balance between androgens and estrogens is very important in the development of prostate, even small changes estrogen levels, including those estrogen-mimicking chemicals, can lead to serious changes. Bisphenol A (BPA), an endocrine-disrupting chemical, a well-known, ubiquitous, estrogenic chemical. To investigate effects fetal exposure low-dose BPA on we examined alterations situ sex steroid hormonal environment mouse urogenital sinus (UGS). In BPA-treated UGS, estradiol (E2) levels...
Nuclear pore complexes (NPCs) on the nuclear membrane surface have a crucial function in controlling movement of small molecules and macromolecules between cell nucleus cytoplasm through their intricate core channel resembling spiderweb with several layers. Currently, there are few methods available to accurately measure dynamics pores membranes at nanoscale. The limitation traditional optical imaging is due diffraction, which prevents achieving required resolution for observing diverse...
Nutritional status is a determining factor for growth during development and homeostatic maintenance in adulthood. In the context of muscle, hormone (GH) coordinates with nutritional status; however, detailed mechanisms remain to be fully elucidated. Here, we show that transcriptional repressor B cell lymphoma 6 (BCL6) maintains muscle mass by sustaining GH action. Muscle-specific genetic deletion BCL6 at either perinatal or adult stages profoundly reduces compromises strength. Conversely,...
Estrogen receptor α (ERα) is pivotal in gene regulation, particularly estrogen-responsive cancers. However, the full-length molecular dynamic structure of ERα remains elusive. In this study, we employ high-speed atomic force microscopy (HS-AFM) to visualize interactions with estrogen response element (ERE) under both ligand-present and ligand-absent conditions. binds ERE even absence estrogen, although presence ligand significantly enhances binding precision stability. Our real-time,...
Bisphenol A and its derivatives are recognized as endocrine disruptors based on their complex effects estrogen receptor (ER) signaling. While the of bisphenol ERα have been thoroughly evaluated, how these chemicals affect ERβ signaling is less well understood. Herein, we sought to identify novel ligands using a radioligand competitive binding assay screen chemical library derivatives. Many compounds identified showed intriguing dual activities both agonists antagonists. Docking simulations...
Probes containing a bioisostere for protein labeling systems using HaloTag and PYP-tag were developed to suppress undesired organelle accumulation applied live-cell imaging of GLUT4.
Halogenated flame retardants comprising bisphenol A (BPA) derivatives, such as tetrabromobisphenol (TBBPA), have been studied their adverse effects on human health. However, despite the fact that these halogenated BPAs are easily degraded in environment, risks to living organisms due products mostly overlooked. To evaluate potential toxicity of TBBPAs and related compounds, we examined cytotoxicity derivatives possessing one four halogen atoms
Bisphenol A, 2,2‐bis(4‐hydroxyphenyl)propane, is an estrogenic endocrine disruptor that influences various physiological functions at very low doses, even though bisphenol A itself ineffectual as a ligand for the estrogen receptor. We recently demonstrated binds strongly to human estrogen‐related receptor γ, one of 48 nuclear receptors. inverse antagonist γ sustain high basal constitutive activity latter and reverse deactivating agonist 4‐hydroxytamoxifen. However, intrinsic binding mode...
Pigment-dispersing factor (PDF), an 18-amino acid neuropeptide, is a principal circadian neuromodulator functioning downstream of the insect brain's clock, modulating daily rhythms locomotor activity. Recently, we found that PDF precursors cricket Gryllus bimaculatus comprise nuclear localization signal (NLS). Moreover, immunoreactivity and trans-location GFP-fused precursor into nucleus have both been demonstrated. These suggest fundamental role for peptide in clock system within nucleus,...
Pigment-dispersing factor (PDF) is a neuropeptide widely distributed in insect brains and plays important roles the circadian system. In this study, we used RNA interference to study role of pigment-dispersing ( pdf) gene regulating locomotor rhythms cricket, Gryllus bimaculatus. Injections pdf double-stranded (ds effectively knocked down mRNA PDF peptide levels. The treated crickets maintained rhythm both under light-dark cycles (LD) constant darkness (DD). However, they showed with reduced...
The endocrine disruptor bisphenol A (BPA) affects various genes and hormones even at merely physiological levels. We recently demonstrated that BPA binds strongly to human nuclear receptor estrogen-related (ERR) γ the phenol-A group of is in a receptacle pocket with essential amino acid residues provide structural support backside. This led bind ERRγ an induced-fit-type binding mode, for example, rotated motion Val313 Tyr326-binding site. similar mechanism appears occur site phenol-B ring....
Abstract Bisphenol A (BPA) is used as an industrial raw material for polycarbonate plastics and epoxy resins; however, various concerns have been reported regarding its status endocrine-disrupting chemical. BPA interacts not only with oestrogen receptors (ERs) but constitutive androstane receptor, pregnane X oestrogen-related receptor γ (ERRγ); therefore, the bisphenol structure represents a privileged nuclear-receptor superfamily. Here, we screen 127 BPA-related compounds by...
Bisphenol A (BPA) strongly binds to human estrogen-related receptor γ (ERRγ). BPA is an oestrogenic endocrine disruptor that influences various physiological functions at very low doses. as inverse-type antagonist of ERRγ retain its high basal constitutive activity by inhibiting the deactivating inverse agonist 4-hydroxytamoxifen (4-OHT). We recently demonstrated residues Glu275 and Arg316 function intrinsic binding site BPA's phenol-hydroxyl group. also determined chief importance...
Various lines of evidence have shown that bisphenol A (BPA) acts as an endocrine disruptor affects various hormones even at merely physiological levels. We demonstrated recently BPA binds strongly to human nuclear receptor estrogen-related γ (ERRγ), one 48 receptors. Based on X-ray crystal analysis the ERRγ ligand-binding domain (LBD)/BPA complex, we residues, Glu275 and Arg316, function intrinsic-binding site phenol–hydroxyl group BPA. If these phenol–hydroxyl↔Glu275 Arg316 hydrogen bonds...
In the ligand/receptor interaction, side chain phenyl group of phenylalanine (Phe) is involved in a so-called hydrophobic which Phe-phenyl functions as p element or merely element. The thrombin receptor-tethered ligand SFLLRNP consists Phe-2 residue essential for receptor activation. order to explore molecular characteristics this Phe-2-phenyl group, complete set S/Phe/LLRNP peptides comprising six different difluorophenylalanine isomers [(F(2))Phe] was newly synthesized and assayed evaluate...