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  • ABOUT
    • About INDIGO
    • Why INDIGO
    • Key Personnel
      • Board of Directors & Advisors
      • Management
    • Employment
    • INDIGO Press Releases
    • INDIGO in the News
  • ASSAYS
    • By Receptor
    • By Disease State
      • Overview
      • Anemia & Kidney Disease
      • Autoimmune Disease & Inflammation
      • Cancer
      • Cardiovascular Disease
      • Diabetes
      • Endocrinology
      • NAFLD/NASH
      • Obesity
    • Toxicology Solutions
      • In Vitro Toxicology Platform
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      • Discovery Toxicology
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    • INDIGlo Luciferase Detection Reagent
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  • TECHNOLOGY
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New Publications

Scientific studies, scholarly articles, and patent information to Nuclear Receptors and Nuclear Receptor research.

Assessment of Herb-Drug Interaction Potential of Five Common Species of Licorice and Their Phytochemical Constituents

ABSTRACT The dried roots and rhizomes of Glycyrrhiza species (G. glabra, G. uralensis and G. inflata), commonly known as licorice, have long been used in traditional medicine. In addition, two other species, G. echinata and G. lepidota are also considered “licorice” in select markets. Currently, licorice is an integral part of several botanical drugs andRead More

Posted in New Publications | Tagged AhR, AhR assay | Comments Off on Assessment of Herb-Drug Interaction Potential of Five Common Species of Licorice and Their Phytochemical Constituents

Characterization of a novel non-steroidal glucocorticoid receptor agonist optimized for topical treatment

ABSTRACT Glucocorticoids (GCs) are commonly used topical treatments for skin diseases but are associated with both local and systemic side effects. In this study, we describe a selective non-steroidal glucocorticoid receptor (GR) agonist for topical use, LEO 134310, which is rapidly deactivated in the blood resulting in low systemic exposure and a higher therapeutic indexRead More

Posted in New Publications | Tagged GR, MR, MR assay | Comments Off on Characterization of a novel non-steroidal glucocorticoid receptor agonist optimized for topical treatment

Towards regulation of Endocrine Disrupting chemicals (EDCs) in water resources using bioassays – A guide to developing a testing strategy

ABSTRACT Endocrine disrupting chemicals (EDCs) are found in every environmental medium and are chemically diverse. Their presence in water resources can negatively impact the health of both human and wildlife. Currently, there are no mandatory screening mandates or regulations for EDC levels in complex water samples globally. Bioassays, which allow quantifying in vivo or inRead More

Posted in New Publications | Tagged AR, EDC, environmental, ERa, ERb, TRa, TRb | Comments Off on Towards regulation of Endocrine Disrupting chemicals (EDCs) in water resources using bioassays – A guide to developing a testing strategy

Human gut bacterial metabolism drives Th17 activation and colitis

ABSTRACT Bacterial activation of T helper 17 (Th17) cells exacerbates mouse models of autoimmunity, but how human-associated bacteria impact Th17-driven disease remains elusive. We show that human gut Actinobacterium Eggerthella lenta induces intestinal Th17 activation by lifting inhibition of the Th17 transcription factor Rorγt through cell- and antigen-independent mechanisms. E. lenta is enriched in inflammatoryRead More

Posted in New Publications | Tagged ROR gamma, ROR gamma assay, RORg | Comments Off on Human gut bacterial metabolism drives Th17 activation and colitis

Bifidobacterium species associated with breastfeeding produce aromatic lactic acids in the infant gut

ABSTRACT Breastfeeding profoundly shapes the infant gut microbiota, which is critical for early life immune development, and the gut microbiota can impact host physiology in various ways, such as through the production of metabolites. However, few breastmilk-dependent microbial metabolites mediating host–microbiota interactions are currently known. Here, we demonstrate that breastmilk-promoted Bifidobacterium species convert aromatic aminoRead More

Posted in New Publications | Tagged AhR, AhR assay | Comments Off on Bifidobacterium species associated with breastfeeding produce aromatic lactic acids in the infant gut

Olive Leaf-Derived PPAR Agonist Complex Induces Collagen IV Synthesis in Human Skin Models

Abstract Introduction Peroxisome proliferator-activated receptor (PPAR) agonists are known to modulate the synthesis of dermal lipids and proteins including collagens. Olive (Olea europaea) leaves have been reported to contain PPAR-binding ligands. Collagen IV, a major dermal-epidermal junction (DEJ) protein, degrades with both age and disease. Here, we report the formulation of a novel multi-ligand complex,Read More

Posted in New Publications | Tagged PPAR alpha assay, PPARa, PPARα | Comments Off on Olive Leaf-Derived PPAR Agonist Complex Induces Collagen IV Synthesis in Human Skin Models

Discovery of 2-(Ortho-Substituted Benzyl)-Indole Derivatives as Potent and Orally Bioavailable RORγ Agonists with Antitumor Activity

Abstract RORγ is a dual-functional drug target, which involves not only induction of inflammation but also promotion of cancer immunity. The development of agonists of RORγ promoting Th17 cell differentiation could provide a novel mechanism of action (MOA) as an immune-activating anticancer agent. Herein, we describe new 2-(ortho-substituted benzyl)-indole derivatives as RORγ agonists by scaffoldRead More

Posted in New Publications | Tagged ROR alpha, ROR alpha assay, RORa, RORg | Comments Off on Discovery of 2-(Ortho-Substituted Benzyl)-Indole Derivatives as Potent and Orally Bioavailable RORγ Agonists with Antitumor Activity

A ready-to-use, thermoresponsive, and extended-release delivery system for the paranasal sinuses

Abstract A drug delivery system for the paranasal sinuses consisting of a freeze-dried thermoresponsive hydrogel with degradable microspheres, called FD-TEMPS (Freeze Dried—Thermogel, Extended-release Microsphere-based delivery to the Paranasal Sinuses), was developed. Glass transition temperatures (Tg′) of the maximally freeze concentrated solutions consisting of poly(N-isopropylacrylamide) (pNIPAAm) and polyethylene glycol (PEG) were determined by differential scanning calorimetry,Read More

Posted in New Publications | Tagged glucocorticoid receptor assay, GR | Comments Off on A ready-to-use, thermoresponsive, and extended-release delivery system for the paranasal sinuses

Discovery of 4-Benzyloxy and 4-(2-Phenylethoxy) Chalcone Fibrate Hybrids as Novel PPARα Agonists with Anti-hyperlipidemic and Antioxidant Activities: Design, Synthesis0020and in Vitro/in Vivo Biological Evaluation

Abstract In the current work, a series of novel 4-benzyloxy and 4-(2-phenylethoxy) chalcone fibrate hybrids (10a-o) and (11a-e) were synthesized and evaluated as new PPARα agonists in order to find new agents with higher activity and fewer side effects. The 2-propanoic acid derivative 10a and the 2-butanoic acid congener 10i showed the best overall PPARαRead More

Posted in New Publications | Tagged PPAR, PPARa, PPARα | Comments Off on Discovery of 4-Benzyloxy and 4-(2-Phenylethoxy) Chalcone Fibrate Hybrids as Novel PPARα Agonists with Anti-hyperlipidemic and Antioxidant Activities: Design, Synthesis0020and in Vitro/in Vivo Biological Evaluation

Withanolide Derivative 2,3-Dihydro-3β-methoxy Withaferin-A Modulates the Circadian Clock via Interaction with RAR-Related Orphan Receptor α (RORa)

Abstract Withanolide derivatives have anticancer, anti-inflammatory, and other functions and are components of Indian traditional Ayurvedic medicine. Here, we found that 2,3-dihydro-3β-methoxy withaferin-A (3βmWi-A), a derivative of withaferin-A (Wi-A) belonging to a class of withanolides that are abundant in Ashwagandha (Withania somnifera), lengthened the period of the circadian clock. This compound dose-dependently elongated circadian rhythmsRead More

Posted in New Publications | Tagged circadian rhythm, Nr1d1, oncology, ROR, ROR alpha, RORa | Comments Off on Withanolide Derivative 2,3-Dihydro-3β-methoxy Withaferin-A Modulates the Circadian Clock via Interaction with RAR-Related Orphan Receptor α (RORa)
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