Scientific studies, scholarly articles, and patent information to Nuclear Receptors and Nuclear Receptor research.
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,
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.
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: G1
Structures and biological activities of new carnosic acid- and carnosol-related compounds generated by heat treatment of rosemary
ABSTRACTCarnosic acid (CA) and carnosol (CS) are components of rosemary reported to possess antioxidative and peroxisome proliferator-activated receptor gamma (PPARγ) transcriptional activities that are useful for preventing metabolic disorders. The aims of this study were to identify new bioactive compounds in heated rosemary and examine their effects on antioxidative stress and PPARγ activation. In heated
ABSTRACT The importance of gut microbiota in human health and pathophysiology is undisputable. Despite the abundance of metagenomics data, the functional dynamics of gut microbiota in human health and disease remain elusive. Urolithin A (UroA), a major microbial metabolite derived from polyphenolics of berries and pomegranate fruits displays anti-inflammatory, anti-oxidative, and anti-ageing activities. Here, we
Rifamycin SV exhibits strong anti-inflammatory in vitro activity through pregnane X receptor stimulation and NFkB inhibition
ABSTRACTRifamycin SV (rifamycin), is a member of the ansamycin family of antimicrobial compounds which kills bacteria commonly associated with infectious diarrhea and other enteric infections. Rifamycin has been found to be effective in experimental animal models of gut inflammation and its efficacy in these settings has been attributed partially to immunomodulatory non-bactericidal activities. This study
Trace organic contaminant removal in six full-scale integrated fixed-film activated sludge (IFAS) systems treating municipal wastewater
ABSTRACT Trace organic contaminants (TrOCs) often pass through conventional activated sludgewastewater treatment plants (CAS-WWTPs) and are discharged into surface waters, where they can threaten aquatic ecosystems and human health, largely due to the hormone disrupting effects of certain TrOCs. The integrated fixed-film activated sludge (IFAS) process is a cost-effective means of upgrading CAS-WWTPs by adding free-floating carrier media, which promotes biofilm formation
Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies Author links open overlay panel
ABSTRACT We previously published on the design and synthesis of novel, potent and selective PPARα antagonists suitable for either i.p. or oral in vivo administration for the potential treatment of cancer. Described herein is SAR for a subsequent program, where we set out to identify selective and potent PPARα/δ dual antagonist molecules. Emerging literature indicates that both
Identification and Molecular Characterization of Peroxisome Proliferator-Activated Receptor δ as a Novel Target for Covalent Modification by 15-Deoxy-Δ12,14-prostaglandin J2
ABSTRACT PPARδ belongs to the peroxisome proliferator-activated receptor (PPAR) family of nuclear receptors. Upon activation by an agonist, PPARδ controls a variety of physiological processes via regulation of its target genes. 15-Deoxy-Δ12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin that features an electrophilic, α,β-unsaturated ketone (an enone) in the cyclopentenone ring. Many of 15d-PGJ2’s biological effects result
ABSTRACT The present application provides novel tetrahydro – isohumulone ( THIAA ) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof . The application further provides methods of using the disclosed compounds and compositions to activate PPARy , inhibit inflammation , and treat conditions associated with inflammation and conditions responsive to PPARY modulation such