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  • HOME
  • ABOUT
    • About
    • Why INDIGO
    • Key Personnel
      • Board of Directors & Advisors
      • Management
  • PRODUCTS
    • Assays
    • Ortholog Assays
    • Growth Factor Receptors
    • In Vitro Toxicology Platform
    • MDR1 / Human P-Glycoprotein
    • Gene Expression
    • NASH Nuclear Receptors For Research
    • Disease States
    • Live Cell Multiplex
    • Custom Assay Development
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New Publications

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

Antisense oligonucleotide development for the selective modulation of CYP3A5 in renal disease

ABSTRACT CYP3A5 is the primary CYP3A subfamily enzyme expressed in the human kidney and its aberrant expression may contribute to a broad spectrum of renal disorders. Pharmacogenetic studies have reported inconsistent linkages between CYP3A5 expression and hypertension, however, most investigators have considered CYP3A5*1 as active and CYP3A5*3 as an inactive allele. Observations of gender specificRead More

Posted in New Publications | Tagged CYP, CYP3A5, Mineralocorticoid Receptor, MR | Comments Off on Antisense oligonucleotide development for the selective modulation of CYP3A5 in renal disease

siRNAs containing 2′-fluorinated Northern-methanocarbacyclic (2′-F-NMC) nucleotides: in vitro and in vivo RNAi activity and inability of mitochondrial polymerases to incorporate 2′-F-NMC NTPs

ABSTRACT We recently reported the synthesis of 2′-fluorinated Northern-methanocarbacyclic (2′-F-NMC) nucleotides, which are based on a bicyclo[3.1.0]hexane scaffold. Here, we analyzed RNAi-mediated gene silencing activity in cell culture and demonstrated that a single incorporation of 2′-F-NMC within the guide or passenger strand of the tri-N-acetylgalactosamine-conjugated siRNA targeting mouse Ttr was generally well tolerated. Exceptions wereRead More

Posted in New Publications | Comments Off on siRNAs containing 2′-fluorinated Northern-methanocarbacyclic (2′-F-NMC) nucleotides: in vitro and in vivo RNAi activity and inability of mitochondrial polymerases to incorporate 2′-F-NMC NTPs

AGONISTS OF PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR ALPHA AND METHODS OF USE

ABSTRACT Benzyl derivative compounds having peroxisome proliferator-activated receptor α (PPARα) agonistic activity, compositions containing such compounds, and methods of their use in enhancing PPARα activity for treating diseases and/or conditions involving inflammation and/or angiogenesis, particularly ocular diseases and/or conditions such as but not limited to retinal inflammation, retinal neovascularization, retinal vascular leakage, retinopathy of prematurity,Read More

Posted in New Publications | Tagged PPAR, PPARa, PPARα, PPARα agonist | Comments Off on AGONISTS OF PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR ALPHA AND METHODS OF USE

Rheum rhaponticum Root Extract Improves Vasomotor Menopausal Symptoms and Estrogen-Regulated Targets in Ovariectomized Rat Model

ABSTRACT Ovarian insufficiency and ovariectomy are characterized by deregulated heat loss mechanisms. Unlike hormone therapy, ERr 731 (a standardized botanical extract of Siberian rhubarb Rheum rhaponticum L. high in rhaponticin) acts like a selective estrogen receptor modulator for ERβ receptors and may offer a higher degree of safety while maintaining the desired efficacy profile. InRead More

Posted in New Publications | Tagged ERa, ERb, estrogen, estrogen receptor, estrogen receptor beta, Estrogen receptor α | Comments Off on Rheum rhaponticum Root Extract Improves Vasomotor Menopausal Symptoms and Estrogen-Regulated Targets in Ovariectomized Rat Model

COMPOSITIONS AND METHODS FOR TREATING CHOLESTATIC DISEASE

ABSTRACT The invention provides compositions and methods for use in the treatment and prevention of cholestatic diseases. To read the full Patent, click HERE. Date of publication: 14 January 2021; United States Patent Application 20210008128 Inventor Information: Nandakumar, Madhumitha (Arlington, MA, US), Liou, Alice Peiyu (Somerville, MA, US), Halvorsen, Elizabeth Moritz (Malden, MA, US), Mckenzie,Read More

Posted in New Publications | Tagged farnesoid X receptor, FXR | Comments Off on COMPOSITIONS AND METHODS FOR TREATING CHOLESTATIC DISEASE

Lipoxygenase catalyzed metabolites derived from docosahexaenoic acid are promising antitumor agents against breast cancer

ABSTRACT Docosahexaenoic acid (DHA) is known to inhibit breast cancer in the rat. Here we investigated whether DHA itself or select metabolites can account for its antitumor action. We focused on metabolites derived from the lipoxygenase (LOX) pathway since we previously showed that they were superior anti-proliferating agents compared to DHA; 4-OXO-DHA was the mostRead More

Posted in New Publications | Tagged PPARg, PPARγ | Comments Off on Lipoxygenase catalyzed metabolites derived from docosahexaenoic acid are promising antitumor agents against breast cancer

A thermoresponsive hydrogel system for long-acting corticosteroid delivery into the paranasal sinuses

ABSTRACT Delivering localized treatment to the paranasal sinuses for diseases such as chronic rhinosinusitis (CRS) is particularly challenging because of the small natural openings leading from the sinuses that can be further obstructed by presence of inflammation. As such, oral steroids, topical nasal sprays or irrigation, and surgery can be utilized to treat persistent sinonasalRead More

Posted in New Publications | Comments Off on A thermoresponsive hydrogel system for long-acting corticosteroid delivery into the paranasal sinuses

Compounds, Compositions, and Methods for Treating Diseases Patent

ABSTRACT The present application is directed, in part, to compounds, and/or pharmaceutically acceptable salts or solvates thereof, and/or pharmaceutical compositions thereof, for modulating the activity of Sigma I receptor. The present application is further directed, in part, to methods for treating and/or preventing cancer using compounds disclosed herein, and/or pharmaceutically acceptable salts or solvates thereof,Read More

Posted in New Publications | Comments Off on Compounds, Compositions, and Methods for Treating Diseases Patent

Synthesis and evaluation of 17α-triazolyl and 9α-cyano derivatives of estradiol

ABSTRACT A variety of 17α-triazolyl and 9α-cyano derivatives of estradiol were prepared and evaluated for binding to human ERβ in both a TR-FRET assay, as well as ERβ and ERα agonism in cell-based functional assays. 9α-Cyanoestradiol (5) was nearly equipotent as estradiol as an agonist for both ERβ and ERα. The potency of the 17α-triazolylestradiolRead More

Posted in New Publications | Tagged ERa, ERb, ERα, ERβ | Comments Off on Synthesis and evaluation of 17α-triazolyl and 9α-cyano derivatives of estradiol

Three-dimensional liver models: state of the art and their application for hepatotoxicity evaluation

ABSTRACT While alternative methods for toxicity testing using re-constructed human skin and cornea have been written into guidelines and adopted by regulatory authorities, three-dimensional (3D) liver models are currently applied in the industrial settings for hepatotoxicity screening and prediction. These 3D liver models can recapitulate the architecture, functionality and toxicity response of the native liver,Read More

Posted in New Publications | Tagged 3D liver model, Hepatocytes, hepatotoxicity, liver injury, spheroid | Comments Off on Three-dimensional liver models: state of the art and their application for hepatotoxicity evaluation
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