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Nuclear Receptor structures

Nuclear Receptor structures. Simon Folkertsma. Nuclear Receptors. ligand-inducible transcription factors ligands are lipophilic compounds 48 human NRs identified key processes are regulated by NRs (homeostasis, dif- ferentiation, embryonic development and organ physiology)

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Nuclear Receptor structures

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  1. Nuclear Receptor structures Simon Folkertsma

  2. Nuclear Receptors • ligand-inducible transcription factors • ligands are lipophilic compounds • 48 human NRs identified • key processes are regulated by NRs (homeostasis, dif- • ferentiation, embryonic development and organ physiology) • diseases: cancer, diabetes, and osteoporosis • Important target for pharmaceutical industry

  3. Domain organization DNA binding domain (DBD) Ligand binding domain (LBD)

  4. Mechanism

  5. 3D Structure NR LBD (hER)

  6. Aligned structures

  7. NR mechanism apo agonist antagonist

  8. Apo

  9. NR mechanism apo agonist antagonist

  10. Agonist

  11. NR mechanism apo agonist antagonist

  12. Antagonist

  13. Where does the ligand bind? • Where is H12? • Where does the cofactor bind? • Is the compound an agonist or antagonist? • Can you find all twelve helices? • Are there hydrogen bonds between the ligand and the • protein?

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