New Publications
Scientific studies, scholarly articles, and patent information to Nuclear Receptors and Nuclear Receptor research.
Detection and Removal of Biologically Active Organic Micropollutants from Hospital Wastewater
ABSTRACT The presence of contaminants of emerging concern (CECs), such as antibiotics, antimicrobial disinfectants, nonprescription drugs, personal care products, pharmaceuticals, and steroids, in water resources can impact aquatic and human health. A large portion of the CECs entering regional wastewater treatment plants originate from hospitals. The purposes of this study were to conduct exploratory analyticalRead More
Quinazolinone derivative BNUA‐3 ameliorated [NDEA+2‐AAF]‐ induced liver carcinogenesis in SD rats by modulating AhR‐CYP1B1‐Nrf2‐Keap1 pathway
ABSTRACT Cytochrome P450 1B1, considered as one of the novel chemotherapeutic targets involved in cancer prevention and therapy is also associated with the conversion of procarcinogens into their active metabolites. The aryl hydrocarbon receptor (AhR) is responsible for mediating different biological responses to a wide variety of environmental pollutants and also causes transcriptional activation ofRead More
Correlation Between Cytochrome P450 Inducers and Nuclear Receptor Activation – a Screening Approach
View Full Size Research conducted by: Shantanu Roychowdhury (1); Casidy M. Ward (1); Kevin J. Kennedy (1); & Yong Zhao (1) (1) Eurofins Discovery, 6 Research Park Drive, St. Charles, MO 63304 Date of Publication: 2019 Presented at: ISSX 2019 in Portland, OR
Intramolecular [2+2] Photocycloaddition of Altrenogest: Confirmation of Product Structure, Theoretical Mechanistic Insight, and Bioactivity Assessment
ABSTRACT While studying the environmental fate of potent endocrine-active steroid hormones, we observed the formation of an intramolecular [2+2] photocycloaddition product (2) with a novel hexacyclic ring system following photolysis of altrenogest (1). The structure and absolute configuration were established by X-ray diffraction analysis. Theoretical computations identified a barrierless two-step cyclization mechanism for the formationRead More
Adverse Outcome Pathway on antagonist binding to PPARa leading to body-weight loss
ABSTRACT The present AOP describes antagonistic chemical binding to the peroxisome proliferator-activated receptor α (PPARα), resulting in preferential binding a co-repressor to the overall PPARα signalling complex causing a chain of events that includes: antagonism of PPARα nuclear signalling, decreased transcriptional expression of PPARα-regulated genes that support energy metabolism, inhibited metabolic energy production (decreased fattyRead More
A synthesis strategy for tetracyclic terpenoids leads to agonists of ERβ
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