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Related Concept Videos

Cholesterol: Significance and Regulation01:29

Cholesterol: Significance and Regulation

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Although not a source of energy, cholesterol plays a significant role as a foundational structure for bile salts, steroid hormones, and vitamin D, as well as being a crucial component of plasma membranes. Approximately 15% of blood cholesterol is derived from our diet, with the remainder synthesized from acetyl CoA by the liver and intestines. Cholesterol is eliminated from the body through its conversion into bile salts, which are eventually discarded in the feces.
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Inverse Trigonometric Functions01:29

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Inverse trigonometric functions are fundamental mathematical tools that reverse the actions of standard trigonometric functions. While trigonometric functions map angles to ratios, inverse trigonometric functions perform the opposite operation by mapping a ratio back to its corresponding angle. These functions are essential in various applications, particularly in determining angles when given specific distances, such as calculating elevation angles in navigation and engineering.For a function...
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Inverse Hyperbolic Functions and Their Derivatives01:25

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The shape of a suspension bridge cable hanging under its own weight is described by a catenary curve, which is modeled using the hyperbolic cosine function. This mathematical model accurately captures the balance between gravity and tension acting along the cable. When a particular vertical position on the cable is known, the corresponding horizontal position can be determined using the inverse hyperbolic cosine function, allowing for a detailed analysis of the cable's geometry.Inverse...
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Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
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A ship tracking an approaching aircraft relies on geometric measurements to find out the aircraft’s position relative to the observer. By measuring the slant distance to the aircraft and the angle of elevation, the horizontal and vertical components of the distance can be obtained using trigonometric relationships. This geometric approach provides a basis for analyzing how the observed angle changes as the aircraft moves closer to the ship.To examine the mathematical behavior of the angle...
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Cholesterol Unbound RORγt Protein Enables a Sensitive Inverse Agonist Screening.

Ryokichi Koyama1, Yasunori Fukuda1, Yusuke Kamada1

  • 11 Biomolecular Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited , Fujisawa, Japan .

Assay and Drug Development Technologies
|June 7, 2018
PubMed
Summary

Researchers identified a new RORγt inverse agonist, compound 1, using a novel screening method. This compound shows promise for treating autoimmune diseases by targeting RORγt (retinoic acid-related orphan receptor gamma T) activity.

Keywords:
RORγtcholesterolhigh-throughput screeninginverse agonistretinoic acid-related orphan receptor gamma T

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Area of Science:

  • Molecular Biology
  • Pharmacology
  • Immunology

Background:

  • Retinoic acid-related orphan receptor gamma T (RORγt) is crucial for Th17 cell function and implicated in autoimmune diseases.
  • RORγt activity is physiologically modulated by cholesterol derivatives, suggesting a therapeutic target.
  • RORγt inverse agonists are potential treatments for Th17-mediated autoimmune conditions like rheumatoid arthritis, asthma, IBD, and psoriasis.

Purpose of the Study:

  • To identify novel RORγt inverse agonists through a high-throughput screening campaign.
  • To evaluate the suitability of apo-RORγt protein for sensitive screening.
  • To characterize the mechanism of action of newly identified inverse agonists.

Main Methods:

  • Comparative analysis of apo-RORγt and cholesterol-bound RORγt using known inverse agonist TO901317.
  • High-throughput screening using a fluorescence-based cholesterol binding assay with apo-RORγt.
  • In vitro assays to assess compound 1's inhibition of RORγt-cholesterol interaction, coactivator recruitment, and transcriptional activity.
  • Cell-based reporter gene assays, including lipid depletion treatment.

Main Results:

  • The known RORγt inverse agonist TO901317 exhibited higher potency against apo-RORγt compared to cholesterol-bound RORγt.
  • High-throughput screening identified compound 1 as a novel cholesterol-competitive RORγt inverse agonist.
  • Compound 1 effectively inhibited RORγt-cholesterol binding, coactivator recruitment, and transcriptional activity.
  • Cell-based assays confirmed compound 1's enhanced potency following lipid depletion.

Conclusions:

  • Apo-RORγt protein is a suitable and sensitive target for high-throughput screening of RORγt inverse agonists.
  • Compound 1 represents a promising novel RORγt inverse agonist with potential therapeutic applications in autoimmune diseases.
  • The findings support a strategy of targeting cholesterol-regulated RORγt for drug discovery.