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Free Whitepaper:

Species Differences in Pregnane X Receptor Activation: Examination of Common Laboratory Animal Species

One nuclear receptor with the ability to associate with a wide range of xenobiotics, including pharmaceutical agents, natural products, and environmental chemicals is pregnane X receptor (PXR). Activation of PXR regulates the expression of xenobiotic metabolizing enzymes such as cytochrome P450 and glutathione-S-transferases, as well as important drug transporters (P-glycoprotein, multidrug resistance protein). The PXR ligand binding domain is unusually divergent across species, compared to other nuclear receptors, with only 50% sequence identity between mammalian and non-mammalian PXR sequences. With such a pronounced difference, the ability to extrapolate human PXR activity from laboratory animal species is an important aspect of addressing the potential of drug-drug interactions with a new drug lead.

In this whitepaper from INDIGO Biosciences, a group of known PXR agonists is examined for their ability to regulate the activity of human, monkey, dog, rat, and mouse orthologues of PXR.

Download this informative resource today for insights on the unique profiles observed for each orthologue of PXR and to learn more about the observed species differences in both potency and efficacy of the chemicals examined.

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This Whitepaper Examines:

  • The amino acid sequences of human, monkey, dog, rat, and mouse PXR
  • The dose response relationships of prototypical PXR ligands
  • The species differences in both potency and efficacy of chemicals on PXR

Download the whitepaper to explore how PXR activation differs across human and common laboratory animal species, with insights into potency, efficacy, and translational relevance.

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INDIGO Biosciences, Inc. is a leading provider of nuclear receptor and in vitro toxicology solutions that accelerate scientific decision-making. We supplement the world’s largest portfolio of nuclear receptor kits and services and in vitro toxicology solutions with greater results readability, reproducibility, and faster turnaround times. Our solutions, plus supportive team and reliable science and platforms, aim to reduce the time, cost, and risk associated with the discovery process.