A5062738635- Estrogen and related hormone effects
- Phytoestrogen effects and research
- Direction-of-Arrival Estimation Techniques
- Effects and risks of endocrine disrupting chemicals
- Computational Drug Discovery Methods
- Microwave Imaging and Scattering Analysis
- Advanced MIMO Systems Optimization
- Synthesis and biological activity
- Cooperative Communication and Network Coding
- Advanced Wireless Communication Techniques
- Sparse and Compressive Sensing Techniques
- Pharmaceutical and Antibiotic Environmental Impacts
- Protein Kinase Regulation and GTPase Signaling
- Genomics, phytochemicals, and oxidative stress
- Speech and Audio Processing
- Cancer Genomics and Diagnostics
- Advanced SAR Imaging Techniques
- Bioactive Compounds and Antitumor Agents
- Radar Systems and Signal Processing
- Retinoids in leukemia and cellular processes
- Cancer, Hypoxia, and Metabolism
- Free Radicals and Antioxidants
- Error Correcting Code Techniques
- Millimeter-Wave Propagation and Modeling
- Ginseng Biological Effects and Applications
Xavier University
2007-2024
Roche (Switzerland)
2022-2023
Xavier University of Louisiana
2012-2022
Empire State University
2022
Louisiana Christian University
2006-2021
Institut für Informationsverarbeitung
2015-2018
Technical University of Munich
2011-2018
Louisiana State University Health Sciences Center New Orleans
2017
University of New Orleans
2016
Tulane University
2001-2012
We present a method for estimating conditionally Gaussian random vectors with covariance matrices, which uses techniques from the field of machine learning. Such models are typical in communication systems, where matrix channel vector depends on parameters, e.g., angles propagation paths. If matrices exhibit certain Toeplitz and shift-invariance structures, complexity MMSE estimator can be reduced to O(M log M) floating point operations, M is dimension. While absence structure much higher,...
Seven legume extracts containing phytoestrogens were analyzed for estrogenic activity. Methanol prepared from soybean (Glycine max L.), green bean (Phaseolus vulgaris alfalfa sprout (Medicago sativa mung (Vigna radiata kudzu root (Pueraria lobata and red clover blossom (Trifolium pratense L.). Extracts of showed significant competitive binding to estrogen receptor beta (ERbeta). Estrogenic activity was determined using an estrogen-dependent MCF-7 breast cancer cell proliferation assay. Kudzu...
Comparative molecular field analysis (CoMFA), a three-dimensional quantitative structure−activity relationship (3D-QSAR) paradigm, was used to examine the estrogen receptor (ER) binding affinities of series structurally diverse natural, synthetic, and environmental chemicals interest. The CoMFA/3D-QSAR model is statistically robust internally consistent, successfully illustrates that overall steric electrostatic properties ligands for are both necessary sufficient describe affinity. ability...
Background Several environmental agents termed "endocrine disrupting compounds" or EDCs have been reported to bind and activate the estrogen receptor-α (ER). The DDT BPA are ubiquitously present in environment, levels human blood adipose tissue detectable most if not all women men. ER-mediated biological responses can be regulated at numerous levels, including expression of coding RNAs (mRNAs) more recently non-coding (ncRNAs). Of ncRNAs, microRNAs emerged as a target signaling. Given...
Alterations in sphingolipid metabolism have been shown to contribute the development of endocrine resistance and breast cancer tumor survival. Sphingosine kinase (SK), particular, is overexpressed a promising target for drug development. In this study, we used novel SK inhibitor ABC294640 as tool explore relationship between estrogen (E2) receptor (ER) signaling cells. Treatment with decreased E2-stimulated ERE-luciferase activity both MCF-7 ER-transfected HEK293 Furthermore, reduced...
Abstract Introduction Despite intensive study of the mechanisms chemotherapeutic drug resistance in human breast cancer, few reports have systematically investigated that underlie to chemotherapy-sensitizing agent tumor necrosis factor (TNF)-α. Additionally, relationship between TNF-α mediated by MEK5/Erk5 signaling and epithelial-mesenchymal transition (EMT), a process associated with promotion invasion, metastasis, recurrence has not previously been investigated. Methods To compare...
Orally bioavailable SERDs may offer greater systemic drug exposure, improved clinical efficacy, and more durable treatment outcome for patients with ER-positive endocrine-resistant breast cancer. We report the design synthesis of a boronic acid modified fulvestrant (5, ZB716), which binds to ERα competitively (IC50 = 4.1 nM) effectively downregulates in both tamoxifen-sensitive tamoxifen-resistant cancer cells. Furthermore, It has superior oral bioavailability (AUC 2547.1 ng·h/mL) mice,...
The flavonoid family of phytochemicals, particularly those derived from soy, has received attention regarding their estrogenic activity as well effects on human health and disease. In addition to these flavonoids other including phytostilbene, enterolactone, lignans, possess endocrine activity. types amounts compounds in soy plants are controlled by both constitutive expression stress-induced biosynthesis. benefits soy-based foods may, therefore, be dependent upon the various hormonally...
Glyceollins, a group of novel phytoalexins isolated from activated soy, have recently been demonstrated to be antiestrogens that bind the estrogen receptor (ER) and inhibit estrogen-induced tumor progression. Our previous publications focused specifically on inhibition formation growth by glyceollin mixture, which contains three isomers (I, II, III). Here, we show mixture is also effective as potential antiestrogenic, therapeutic agent prevents estrogen-stimulated tumorigenesis displays...
Recently, crosstalk between sphingolipid signaling pathways and steroid hormones has been illuminated as a possible therapeutic target. Sphingosine kinase (SK), the key enzyme metabolizing pro-apoptotic ceramide to pro-survival sphingosine-1-phosphate (S1P), is promising target for solid tumor cancers. In this study, we examined ability of pharmacological inhibition S1P formation block estrogen targeted breast cancer therapy. We found that Sphk1/2 selective inhibitor (SK (SKI))-II, blocked...
Abstract Alkylated polycyclic aromatic hydrocarbons (APAHs) are abundant in petroleum, but data regarding their toxicological properties limited. A survey of all monomethylated phenanthrene structures revealed that they were 2 times to 5 more potent than for activation human aryl hydrocarbon receptor a yeast bioassay. Phenanthrenes with equatorial methyl groups had the greatest potency. The greater potency methylated phenanthrenes highlights need on APAHs. Environ Toxicol Chem...
With special properties such as excellent fluoresce features, low toxicity, good biocompatibility, permeability, and easy clearance from the body, carbon dot (CD)-based nanoparticles (NPs) have potential to deliver drugs use in vivo diagnostics through molecular imaging. In this work, folic acid-CD (FA-CD) NPs were prepared doxorubicin (Dox) covalently noncovalently cancer theranostics. FA was conjugated surface of CDs for targeting cells with overexpressing folate receptors. various amounts...
Analogues of estradiol-17β (E2) have been evaluated for estrogen receptor (ER) binding affinity and mitogenic potential in the human breast cancer cell line MCF-7. These 42 compounds represent subtle modifications natural structure through placement hydroxyl, amino, nitro, or iodo groups around ring system addition to, as replacement of, 3- 17β-hydroxyls E2. The activity analogues was found to be related ER only a limited extent. In order elucidate structural features that are uniquely...
The primary induced isoflavones in soybean, the glyceollins, have been shown to be potent estrogen antagonists vitro and vivo. discovery of glyceollins' ability inhibit cancer cell proliferation has led analysis estrogenic activities other isoflavones. In this study, we investigated a novel isoflavone, glycinol, precursor glyceollin that is produced elicited soy. Sensitive specific bioassays were used determine glycinol exhibits activity. Estrogen-based reporter assays performed, displayed...
Daidzein (1) is a natural estrogenic isoflavone. We report here that 1 can be transformed into anti-estrogenic ligands by simple alkyl substitutions of the 7-hydroxyl hydrogen. To test effect such structural modifications on hormonal activities resulting compounds, series daidzein analogues have been designed and synthesized. When MCF-7 cells were treated with analogues, those from hydrogen substitution isopropyl (3d), isobutyl (3f), cyclopentyl (3g), pyrano- (2) inhibited cell...
The organochlorine dichlorodiphenyltrichloroethane (DDT), a known estrogen mimic and endocrine disruptor, has been linked to animal human disorders. However, the detailed mechanism(s) by which DDT affects cellular physiology remains incompletely defined.We others have shown that activates cell-signaling cascades, culminating in activation of receptor-dependent -independent gene expression. Here, we identify mechanism alters signaling expression, independent receptor.We performed quantitative...
Development of orally bioavailable nonsteroidal selective estrogen receptor downregulators (SERDs) provides clinical opportunities for the long-term treatment and adjuvant therapy breast cancer at all stages. We describe design, synthesis, identification a boron-modified GW7604 derivative (GLL398, 9), SERD candidate, in which boronic acid functional group replaces phenolic hydroxyl GW7604. Compound 9 strongly binds to ERα fluorescence resonance energy transfer binding assay (IC50 = 1.14 nM)...
Advances in oral SERDs development so far have been confined to nonsteroidal molecules such as those containing a cinnamic acid moiety, which are earlystage clinical evaluation. ZB716 was previously reported an orally bioavailable SERD structurally analogous fulvestrant. In this study, we examined the binding details of estrogen receptor alpha (ERα) by computer modeling reveal its interactions with ligand domain steroidal molecule. We also found that modulates ERα-coregulator nearly...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTInfluence of estrogen structure on nuclear binding and progesterone receptor induction by the complexJ. A. VanderKuur, T. Wiese, S. C. BrooksCite this: Biochemistry 1993, 32, 27, 7002–7008Publication Date (Print):July 1, 1993Publication History Published online1 May 2002Published inissue 1 July 1993https://pubs.acs.org/doi/10.1021/bi00078a027https://doi.org/10.1021/bi00078a027research-articleACS PublicationsRequest reuse permissionsArticle...
As a public health problem, prostate cancer engenders huge economic and life-quality burden. Developing effective chemopreventive regimens to alleviate the burden remains major challenge. Androgen signaling is vital development progression of cancer. Targeting androgen via blocking production potent ligand dihydrotestosterone has been shown decrease incidence. However, potential increasing incidence high-grade cancers concern. Mechanisms disease after intervention may include increased...
In humans, cytochrome P450 1A2 is the major enzyme metabolizing environmental arylamines or heterocyclic amines into carcinogens. Since evidence shows that planar triangle-shaped molecules are capable of selectively inhibiting 1A2, 16 triangular flavone, and coumarin derivatives were designed synthesized for these studies. Among compounds, 7,8-furanoflavone time-dependently inhibits with a KI value 0.44 μM. With 5 min preincubation in presence NADPH, 0.01 μM completely inactivates but does...