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  • HOME
  • ABOUT
    • About
    • Why INDIGO
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      • Management
  • PRODUCTS
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New Publications

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

Cellular Stress Upregulates Indole Signaling Metabolites in Escherichia coli

ABSTRACT Escherichia coli broadly colonize the intestinal tract of humans and produce a variety of small molecule signals. However, many of these small molecules remain unknown. Here, we describe a family of widely distributed bacterial metabolites termed the “indolokines.” In E. coli, the indolokines are upregulated in response to a redox stressor via aspC and tyrB transaminases. Although indolokine 1 represents a previouslyRead More

Posted in New Publications | Tagged antibiotic tolerance, e. coli, host-bacteria interactions, indole, innate immunity, persister cell, signaling, stress response | Comments Off on Cellular Stress Upregulates Indole Signaling Metabolites in Escherichia coli

Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders

ABSTRACT Peroxisome proliferator-activated receptor alpha (PPARα) is expressed in retinal Müller cells, endothelial cells, and in retinal pigment epithelium; agonism of PPARα with genetic or pharmacological tools ameliorates inflammation, vascular leakage, neurodegeneration, and neovascularization associated with retinal diseases in animal models. As such, PPARα is a promising drug target for diabetic retinopathy and age-related macularRead More

Posted in New Publications | Tagged PPARa, PPARα, PPARα agonist, retinal disorders | Comments Off on Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders

Breastmilk-promoted bifidobacteria produce aromatic lactic acids in the infant gut

ABSTRACT Breastfeeding profoundly shapes the infant gut microbiota, which is critical for early life immune development. However, few breastmilk-dependent microbial metabolites mediating host-microbiota interactions are currently known. We here demonstrate that breastmilk-promoted Bifidobacterium species convert aromatic amino acids (tryptophan, phenylalanine and tyrosine) into their respective aromatic lactic acids (indolelactate, phenyllactate and 4-hydroxyphenyllactate) via a previouslyRead More

Posted in New Publications | Tagged AhR, aryl hydrocarbon receptor | Comments Off on Breastmilk-promoted bifidobacteria produce aromatic lactic acids in the infant gut

Structure Based Multitargeted Molecular Docking Analysis of Selected Furanocoumarins against Breast Cancer

ABSTRACT Breast cancer is one of the biggest global dilemmas and its current therapy is to target the hormone receptors by the use of partial agonists/antagonists. Potent drugs for breast cancer treatment are Tamoxifen, Trastuzumab, Paclitaxel, etc. which show adverse effects and resistance in patients. The aim of the study has been on certain phytochemicalsRead More

Posted in New Publications | Tagged breast cancer, EGFR, ER alpha, ERa, mTOR, PGR | Comments Off on Structure Based Multitargeted Molecular Docking Analysis of Selected Furanocoumarins against Breast Cancer

Identifying qualitative differences in PPARα signaling networks in human and rat hepatocytes and their significance for next generation chemical risk assessment methods

ABSTRACT In this paper, we evaluate the PPARα signaling network in rats, examining transcriptional responses in primary hepatocytes exposed to a PPARα specific ligand, GW7647. These transcriptomic studies were complemented with ChIP-seq studies of PPARα binding and transcription binding motif identification for PPARα responsive genes. We also conducted a limited study of GW7647 dosing the inRead More

Posted in New Publications | Tagged fit-for-purpose assays, gene expression profiling, in vitro risk assessment, ortholog, PPARα ChIP-seq, PPARα signaling network, TT221C | Comments Off on Identifying qualitative differences in PPARα signaling networks in human and rat hepatocytes and their significance for next generation chemical risk assessment methods

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

Posted in New Publications | Tagged AR, environmental, ER beta, ERβ, micropollutants, MR, wastewater | Comments Off on Detection and Removal of Biologically Active Organic Micropollutants from Hospital Wastewater

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

Posted in New Publications | Tagged AhR, CYP1B1, FESEM, hepatocellular carcinogenesis, NDEA+ 2-AAF, ortholog, SD rats | Comments Off on Quinazolinone derivative BNUA‐3 ameliorated [NDEA+2‐AAF]‐ induced liver carcinogenesis in SD rats by modulating AhR‐CYP1B1‐Nrf2‐Keap1 pathway

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

Posted in New Publications, Posters | Tagged AhR, CAR, cyp450 inducer, cytochrome p450, PXR | Comments Off on Correlation Between Cytochrome P450 Inducers and Nuclear Receptor Activation – a Screening Approach

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

Posted in New Publications | Tagged androgen receptor, AR, endocrine-active steroid hormones, er, estrogen receptor, pregnane x receptor, PXR | Comments Off on Intramolecular [2+2] Photocycloaddition of Altrenogest: Confirmation of Product Structure, Theoretical Mechanistic Insight, and Bioactivity Assessment

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

Posted in New Publications | Tagged Adverse Outcome Pathway, AOP, body weight loss, PPAR antagonist, PPARa, PPARα | Comments Off on Adverse Outcome Pathway on antagonist binding to PPARa leading to body-weight loss
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