Ligand metabolism and transport - Types of nuclear receptors

4 important questions on Ligand metabolism and transport - Types of nuclear receptors

What is the difference between nuclear receptors and Aryl hydrocarbon receptors (AhR)?

  • Binding place to the DNA
  • Types of dimers
Nuclear receptors: broad sensors, respond to endogenous and exogenous ligands
AhR: specialized xenobiotic sensor, mainly regulating Phase I detoxification enzymes.

What do we specifically know about AhR?

Dioxin response = metaal productie.

What is an important type belonging to the NR1 family? Name 6 characteristics.

PPAR: Peroxisome proliferator activated receptors.
  1. Dimerises with RXR = Retinoid X receptor
  2. Regulated lipid homeostasis and energy metabolism and anti inflammatory responses
  3. The ligand is a fatty acid
  4. In toxicology it binds with PFOA (perfluorooctanoic acid)
  5. In pharmacology it interacts with fibrates and thiazolidinediones
  6. There are 3 types: alpha, gamma, Beta
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Say something about the pharmacological role of PPAR.

  • Fibraten ligand voor PPAR alpha
  • Fibraten (drugs) activate the fatty acid oxidatie (vetverbranding).
  • Verlagen de hoeveelheid triglyceriden (is iets anders dan cholesterol)
  • Minder triglyceriden => minder VLDL nodig (very low density lipoprotein, belangrijk voor het transport)

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