Treatment of hyperthyroidism, a common clinical condition that can have serious manifestations in the elderly, has remained essentially unchanged for >30 years. Directly antagonizing effect thyroid hormone at receptor level may be significant improvement treatment hyperthyroid patients. We built computer model (TR) ligand-binding domain its predicted antagonist-bound conformation and used virtual screening algorithm to select 100 TR antagonist candidates out library >250,000 compounds....

Fluence dependent fluorescence correlation spectroscopy for elucidation of Cu-doping-induced suppression Auger recombination in aqueous CdS quantum dots.

We previously reported that expression of NRIF3 (nuclear receptor interacting factor-3) rapidly and selectively leads to apoptosis breast cancer cells. DIF-1 (also known as interferon regulatory factor-2 binding protein 2 [IRF-2BP2]), the cellular target NRIF3, was identified a transcriptional repressor, knockdown cells but not other cell types. Here, we identify IRF-2BP1 EAP1 (enhanced at puberty 1) important components complex mediating both stability repression. This interaction DIF-1,...

Farnesyl pyrophosphate (FPP), a key intermediate in the mevalonate pathway and protein farnesylation, can act as an agonist for several nuclear hormone receptors. Here we show novel mechanism by which FPP inhibits wound healing acting glucocorticoid receptor (GR). Elevation of endogenous squalene synthetase inhibitor zaragozic acid A (ZGA) or addition to cell culture medium results activation translocation GR, known inhibitor. We used functional studies evaluate effects on healing. Both ZGA...

A comprehensive understanding of exciton dynamics water-soluble quantum dots (QDs), especially those synthesized directly in aqueous media, is critical for devising their applications. Trapping processes are expected to play a pivotal role here, as surface trap states abundant such QDs. The present study, based on ultrafast transient absorption, provides insight into PEI-capped CdS QDs by one-pot reaction water. They robust and strongly photoluminescent (PL), unlike many other Excitation...

Metal chalcogenide quantum dots (QDs) are attractive because of their application in photovoltaics and light emitting devices (LEDs). Non‐radiative Auger recombination is a major hindrance this regard. Doping with metal ions an effective modality to overcome issue. In the present work, effect Cu(I) doping supressing nonradiative MPA‐capped CdS QDs aqueous medium examined as evidenced by ultrafast transient absorption spectroscopy femtosecond optical gating. Doped have shown significant...

Nuclear hormone receptor coregulator (NRC) is a 2,063-amino-acid of nuclear receptors and other transcription factors (e.g., c-Fos, c-Jun, NF-kappaB). We others have generated C57BL/6-129S6 hybrid (C57/129) NRC(+/-) mice that appear outwardly normal grow reproduce. In contrast, homozygous deletion the NRC gene embryonic lethal. NRC(-/-) embryos are always smaller than NRC(+/+) embryos, die between 8.5 12.5 days postcoitus (dpc), suggesting has pleotrophic effect on growth. To study this, we...

The prospect of aqueous polyethyleneimine-capped CdS quantum dots (QDs), in toxic metal-ion sensing, has been explored. Pb2+ binds strongly to the surface QDs facilitating ultrafast electron transfer. As a result, severe (∼90%) PL quenching is observed. Hot transfer plays an important role process, as elucidated by anticorrelation between magnitude ground-state bleach and concentration ions, well concurrent decrease rise time. A second major contribution from conduction band edge, with rate...

Abstract Expression of the nuclear receptor interacting factor 3 (NRIF3) coregulator in a wide variety breast cancer cells selectively leads to rapid caspase-2–dependent apoptotic cell death. A novel death domain (DD1) was mapped 30–amino acid region NRIF3. Because cytotoxicity NRIF3 and DD1 seems be type–specific, these studies suggest that contain “death switch” can specifically modulated by or DD1. Using an MCF-7 cDNA library yeast two-hybrid screen, we cloned mediates apoptosis refer...

A novel method has been reported to deposit low molecular weight organic materials by a layer-by-layer self-assembled film deposition method. different electrostatic adsorption process followed show its advantage over the conventional When an material, namely, alizarin violet, with fewer ionic groups was used as anion for self-assembly, dye found come off during subsequent polycation deposition. As alternative approach, anchored via physiabsorption prior By controlling concentration ratio of...

In silico docking of a chemical library with the ligand-binding domain thyroid hormone nuclear receptor-beta (TRbeta) suggested that farnesyl pyrophosphate (FPP), key intermediate in cholesterol synthesis and protein farnesylation, might function as an agonist. Surprisingly, addition FPP to cells activated TR well classical steroid receptors but not peroxisome proliferative-activating receptors, farnesoid X receptor, liver or several orphan ligands which are unknown. enhanced...

Many anticancer drugs kill cancer cells by inducing apoptosis. Despite the progress in understanding apoptosis, how to harness cellular death machinery selectively deliver tumor-specific cytotoxicity (while minimizing damage other cells) remains an important challenge. We report here that expression of NRIF3 family transcriptional coregulators a variety breast cell lines induces rapid and profound apoptosis (nearly 100% within 24 h). A novel domain (DD1) was mapped short 30-amino-acid region...

Expression of NRIF3 (Nuclear Receptor Interacting Factor-3) rapidly and selectively leads to apoptosis breast cancer cells. This occurs through binding or its 30 amino acid Death Domain-1 (DD1) region the transcriptional repressor, DIF-1 (DD1 Factor-1). acts in a wide variety cells but not other cell types repress pro-apoptotic gene, FASTKD2. DD1 inactivates repressor leading rapid derepression FASTKD2, which initiates within 5–8 h expression. Although FASTKD2 is an inner mitochondrial...

Nonionic surfactant modulated aggregation induced emission enhancement (AIEE) of Dimethyl-2,5-bis(4-(methoxyphenyl)amino)terephthalate (DBMPT) has been investigated. DBMPT exhibits unidirectional aggregated growth with nonionic triton X-100 (TX-100) to produce highly luminescent nanorods, the dimensions and intensities which are controlled by concentration DBMPT. Energy transfer from perylene-3,4,9,10-tetracarboxylic acid dianhydride (PTAD) these nanorods in aqueous medium produces pure...

A series of ruthenium complexes, namely, [{1-(N-R1-2-acetamido)-3-(R2)-benzimidazol-2-ylidine}Ru(p-cymene)Cl]Cl, where {R1 = 2,6-(i-Pr)2C6H3, R2 i-Pr (1c); R1 Et (2c); 2,4,6-(CH3)3C6H2, (3c)}, benzimidazole-derived N/O-functionalized N-heterocyclic carbene ligands successfully carried out the cyanosilylation reaction aromatic aldehydes and heteroaryl with trimethylsilyl cyanide, providing good to excellent yields (ca. 60-95%) at room temperature under solvent-free condition. The (1-3)c...

Targeting tumor DNA damage and p53 pathway is a clinically established strategy in the development of cancer chemotherapeutics. Majority anti-cancer drugs are delivered through parenteral route for reasons like severe toxicity, lack stability, poor enteral absorption. Current targeting clinical anthracycline suffers from major drawbacks cardiotoxicity. Here, we report identification new orally active small molecule curcumin-triazole conjugate (CT-1) with significant anti-breast activity...

Dynamics of preferential solvation 5-aminoquinoline (5AQ) has been studied in hexane-alcohol solvent mixtures. Significant spectral red shift and fluorescence quenching are observed, even for miniscule amounts alcohols. A nonlinear variation these parameters, with alcohol mole fraction, indicates dipolar enrichment around 5AQ its excited state. nanosecond rise at the end emission spectra is ascribed to translational diffusion molecules consequent 5AQ. Electrostatic stabilization hydrogen...

Ultrafast hole capture by dopant Cu + ions leads to intense, red shifted and long-lived photoluminescence in doped tetrapod-shaped CdSe nanoparticles.

Transient characteristics of organic light-emitting devices with alizarin violet as emitting material have been studied. A sequence two voltage pulses separated by a time delay was applied. From the transient response electroluminescence, effects accumulated and injected carriers out. During first pulse, intrinsically charges generated peak in luminance, which absent during latter pulses. The separation between has varied to study relaxation dynamics carriers. By varying molar concentration...

Herein, we report the synthesis of fluorescent 1,4-dihydropyridine-linked bis-triazoles (2a–2n) through Hantzsch by condensation o/m-chloro-substituted benzaldehyde, ethyl 3-oxo-4(prop-2-yn-1-yloxy)butanoate, and ammonium acetate in presence Ba(NO3)2 as a catalyst followed click reaction resultant product (1) with various aromatic well aliphatic azides. All synthesized compounds were characterized 1H-NMR, 13C-NMR, FTIR, HRMS spectral techniques. Antibreast cancer evaluation all derivatives...

The fluorescence of 5-aminoquinoline (5AQ) is quenched strongly in alcoholic solvents, stark contrast to the enhancement observed earlier for its positional isomer, 3-aminoquinoline (3AQ). This phenomenon has been explained by involvement a highly dipolar excited state, which manifested solvatochromism 5AQ. A marked wavelength dependence decays 5AQ solvents ascribed ultrafast solvation state these solvents. resultant stabilization this leads decrease gap between energy and lower lying...