ABSTRACT Natural product and natural product-like molecules continue to be important for the development of pharmaceutical agents, as molecules in this class play a vital role in the pipeline for new therapeutics. Among these, tetracyclic terpenoids are privileged, with >100 being FDA-approved drugs. Despite this significant pharmaceutical success, there remain considerable limitations to broad medicinalRead More
Nuclear Receptors Regulate Intestinal Inflammation in the Context of IBD
ABSTRACT Gastrointestinal (GI) homeostasis is strongly dependent on nuclear receptor (NR) functions. They play a variety of roles ranging from nutrient uptake, sensing of microbial metabolites, regulation of epithelial intestinal cell integrity to shaping of the intestinal immune cell repertoire. Several NRs are associated with GI pathologies; therefore, systematic analysis of NR biology, the underlyingRead More
Characterization of EDP-305, a Highly Potent and Selective Farnesoid X Receptor Agonist, for the Treatment of Non-alcoholic Steatohepatitis
ABSTRACT Non-alcoholic steatohepatitis (NASH), characterized by hepatocyte injury, inflammation, and fibrosis, is the maincause of chronic liver disease in the Western world. There are currently no approved pharmacological therapies for NASH,underscoring the urgent need for effective treatments. The farnesoid X receptor (FXR) has emerged as an attractive target for the treatment of metabolic and chronicRead More
Mechanism and therapeutic window of a genistein nanosuspension to protect against hematopoietic-acute radiation syndrome
ABSTRACT There are no FDA-approved drugs that can be administered prior to ionizing radiation exposure to prevent hematopoietic–acute radiation syndrome (H-ARS). A suspension of synthetic genistein nanoparticles was previously shown to be an effective radioprotectant against H-ARS when administered prior to exposure to a lethal dose of total body radiation. Here we aimed to determineRead More
Metadichol® A Novel Inverse Agonist of Thyroid Receptor and its Application in Thyroid Diseases
ABSTRACT An estimated 200 million individuals worldwide have a thyroid disorder. Thyroid diseases affect seven times more women than men. People not diagnosed make up the majority of thyroid patients. There is a need to find novel and safe ways to change the underlying disease processes, rather than merely stop excess thyroid hormone production asRead More
Bioactive Rearrangement Products from Aqueous Photolysis of Pharmaceutical Steroids
ABSTRACT In an ongoing effort to study the environmental fate of endocrine-active steroid hormones, we report the formation of phenolic rearrangement products (3 and 4) with a novel 6,5,8,5-ring system following aqueous photolysis of dienogest (1) and methyldienolone(2). The structures were established by analysis of 2D NMR and HRMS data, and that of 3 wasRead More
Quizalofop-p-ethyl induces adipogenesis in 3T3-L1 adipocytes
ABSTRACT Exposure to endocrine disrupting chemicals is an established risk factor for obesity. The most commonly used pesticide active ingredients have never been tested in an adipogenesis assay. We tested for the first time the potential of glyphosate, 2,4-dichlorophenoxyacetic acid, dicamba, mesotrione, isoxaflutole and quizalofop-p-ethyl (QpE) to induce lipid accumulation in murine 3T3-L1 adipocytes. OnlyRead More
Synthesis and characterization of hydrogen peroxide activated estrogen receptor beta ligands
ABSTRACT The development and evaluation of selective estrogen receptor modulators (SERMs) is of interest because of the complex and significant role of estrogen receptors in normal tissues as well as disease states. In neurodegenerative disorders such as Alzheimer’s disease and multiple sclerosis, estrogen receptor beta (ERβ) seems to provide a protective anti-inflammatory response. Due toRead More
Cosmetic Composition and Method of Treating the Skin: Patent Application
ABSTRACT A compound that has retinol like properties is used in compositions for treating the skin. To view the rest of the patent application click HERE. Patent Application Number: 16/129,179 Filing Date: 12 September 2018 Publication Date: 28 March 2019 Applicant information: Johnson & Johnson Consumer Inc., Skillman, NJ (US) Inventor information: Cecilia Brun (SaintRead More
Nuclear Receptors & Endocrine / Metabolic Disruption
From our understanding today, there are many environmental chemicals that carry the potential to affect the endocrine system. Known as endocrine disrupting chemicals (EDCs), these compounds alter drug and xenobiotic metabolic processes and can interfere with the production, release, metabolism, and elimination of natural hormones. Through the examination of suspected endocrine and metabolic disruptors andRead More