New Publications
Scientific studies, scholarly articles, and patent information to Nuclear Receptors and Nuclear Receptor research.
COMPOSITIONS AND METHODS FOR TREATING CHOLESTATIC DISEASE
ABSTRACT The invention provides compositions and methods for use in the treatment and prevention of cholestatic diseases. To read the full Patent, click HERE. Date of publication: 14 January 2021; United States Patent Application 20210008128 Inventor Information: Nandakumar, Madhumitha (Arlington, MA, US), Liou, Alice Peiyu (Somerville, MA, US), Halvorsen, Elizabeth Moritz (Malden, MA, US), Mckenzie,Read More
Lipoxygenase catalyzed metabolites derived from docosahexaenoic acid are promising antitumor agents against breast cancer
ABSTRACT Docosahexaenoic acid (DHA) is known to inhibit breast cancer in the rat. Here we investigated whether DHA itself or select metabolites can account for its antitumor action. We focused on metabolites derived from the lipoxygenase (LOX) pathway since we previously showed that they were superior anti-proliferating agents compared to DHA; 4-OXO-DHA was the mostRead More
A thermoresponsive hydrogel system for long-acting corticosteroid delivery into the paranasal sinuses
ABSTRACT Delivering localized treatment to the paranasal sinuses for diseases such as chronic rhinosinusitis (CRS) is particularly challenging because of the small natural openings leading from the sinuses that can be further obstructed by presence of inflammation. As such, oral steroids, topical nasal sprays or irrigation, and surgery can be utilized to treat persistent sinonasalRead More
Compounds, Compositions, and Methods for Treating Diseases Patent
ABSTRACT The present application is directed, in part, to compounds, and/or pharmaceutically acceptable salts or solvates thereof, and/or pharmaceutical compositions thereof, for modulating the activity of Sigma I receptor. The present application is further directed, in part, to methods for treating and/or preventing cancer using compounds disclosed herein, and/or pharmaceutically acceptable salts or solvates thereof,Read More
Synthesis and evaluation of 17α-triazolyl and 9α-cyano derivatives of estradiol
ABSTRACT A variety of 17α-triazolyl and 9α-cyano derivatives of estradiol were prepared and evaluated for binding to human ERβ in both a TR-FRET assay, as well as ERβ and ERα agonism in cell-based functional assays. 9α-Cyanoestradiol (5) was nearly equipotent as estradiol as an agonist for both ERβ and ERα. The potency of the 17α-triazolylestradiolRead More
Three-dimensional liver models: state of the art and their application for hepatotoxicity evaluation
ABSTRACT While alternative methods for toxicity testing using re-constructed human skin and cornea have been written into guidelines and adopted by regulatory authorities, three-dimensional (3D) liver models are currently applied in the industrial settings for hepatotoxicity screening and prediction. These 3D liver models can recapitulate the architecture, functionality and toxicity response of the native liver,Read More
Bacterial metabolism of bile acids promotes generation of peripheral regulatory T cells
ABSTRACT Intestinal health relies on the immunosuppressive activity of CD4+ regulatory T (Treg) cells. Expression of the transcription factor Foxp3 defines this lineage, and can be induced extrathymically by dietary or commensal-derived antigens in a process assisted by a Foxp3 enhancer known as conserved non-coding sequence 1 (CNS1). Products of microbial fermentation including butyrate facilitate the generationRead More
Cellular Stress Upregulates Indole Signaling Metabolites in Escherichia coli
ABSTRACT Escherichia coli broadly colonize the intestinal tract of humans and produce a variety of small molecule signals. However, many of these small molecules remain unknown. Here, we describe a family of widely distributed bacterial metabolites termed the “indolokines.” In E. coli, the indolokines are upregulated in response to a redox stressor via aspC and tyrB transaminases. Although indolokine represents aRead More
Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders
ABSTRACT Peroxisome proliferator-activated receptor alpha (PPARα) is expressed in retinal Müller cells, endothelial cells, and in retinal pigment epithelium; agonism of PPARα with genetic or pharmacological tools ameliorates inflammation, vascular leakage, neurodegeneration, and neovascularization associated with retinal diseases in animal models. As such, PPARα is a promising drug target for diabetic retinopathy and age-related macularRead More
Breastmilk-promoted bifidobacteria produce aromatic lactic acids in the infant gut
ABSTRACT Breastfeeding profoundly shapes the infant gut microbiota, which is critical for early life immune development. However, few breastmilk-dependent microbial metabolites mediating host-microbiota interactions are currently known. We here demonstrate that breastmilk-promoted Bifidobacterium species convert aromatic amino acids (tryptophan, phenylalanine and tyrosine) into their respective aromatic lactic acids (indolelactate, phenyllactate and 4-hydroxyphenyllactate) via a previouslyRead More