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
Safety evaluation of 2′-deoxy-2′-fluoro nucleotides in GalNAc-siRNA conjugates
ABSTRACT For oligonucleotide therapeutics, chemical modifications of the sugar-phosphate backbone are frequently used to confer drug-like properties. Because 2′-deoxy-2′-fluoro (2′-F) nucleotides are not known to occur naturally, their safety profile was assessed when used in revusiran and ALN-TTRSC02, two short interfering RNAs (siRNAs), of the same sequence but different chemical modification pattern and metabolic stability,Read More
Intestinal TGR5 agonism improves hepatic steatosis and insulin sensitivity in Western diet-fed mice
ABSTRACT Takeda G protein-coupled receptor 5 (TGR5) agonists induce systemic release of glucagon-like peptides (GLPs) from intestinal L cells, a potentially therapeutic action against metabolic diseases such as nonalcoholic steatohepatitis (NASH), nonalcoholic fatty liver disease (NAFLD), and Type 2 diabetes. Historically, TGR5 agonist use has been hindered by side effects, including inhibition of gallbladder emptying.Read More
Benzothiophene estrogen receptor modulators: Patent Application
ABSTRACT This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt or a pharmaceutically acceptable composition thereof to treat an estrogen-related medical disorder. To view the rest of the patent application click HERE. Patent Application Number: 15/893295 Filing Date: 09 February 2018 Publication Date: 19 February 2019 Applicant & Assignee information: G1Read More