MPharm Programme: Receptor Superfamilies - Nuclear Receptors
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Questions and Answers

What can lead to systemic organ dysfunction and disease, including inflammation, cancer, diabetes, cardiovascular disease, obesity, and reproductive disorders?

  • Bone growth abnormalities
  • Lipid metabolism disruption
  • Apoptosis dysfunction
  • Mutations, misfolding, or alteration of signaling pathways (correct)

    • Which nuclear receptor is essential for male sexual differentiation, bone growth, muscle homeostasis, and development?

  • Progesterone Receptor (PR)
  • Oestrogen Receptor (ER)
  • Retinoid X Receptor (RXR)
  • Androgen Receptor (AR) (correct)

    • What role does the Progesterone Receptor (PR) play in the body?

  • Muscle homeostasis maintenance
  • Female reproduction
  • Development of mammary glands & other female reproductive organs (correct)
  • Bone growth regulation

    • Which nuclear receptor is associated with breast cancer development & metastasis when dysregulated?

    <p>Oestrogen Receptor (ER)</p> Signup and view all the answers

    What functions are promoted by downregulation or loss of RXR signaling?

    <p>Inflammation of vital organ systems</p> Signup and view all the answers

    Which nuclear receptor plays a key role in lipid metabolism, apoptosis, and the immune system?

    <p>Retinoid X Receptors (RXRs)</p> Signup and view all the answers

    What is a common consequence of dysregulation of nuclear receptor signaling in the body?

    <p>Cancer progression</p> Signup and view all the answers

    What is the initial event in the activation of Class I nuclear receptors?

    <p>Binding of steroid hormone</p> Signup and view all the answers

    What is the final step in the activation pathway of Class I nuclear receptors?

    <p>Binding to hormone response elements on DNA</p> Signup and view all the answers

    Which subclassification of nuclear receptors generally requires ligand binding for both partners to activate?

    <p>TR-RXR</p> Signup and view all the answers

    What is the role of co-repressor complexes like NCoR and SMRT in Class II nuclear receptor signaling?

    <p>Confer ligand-independent repression when bound to heterodimers</p> Signup and view all the answers

    Which nuclear receptor superfamily plays a significant role in lipid metabolism and inflammatory signaling?

    <p>Class II NRs</p> Signup and view all the answers

    How do Class II nuclear receptors like PPAR-RXR and LXR-RXR differ in their ligand binding requirements?

    <p>'Permissive' complexes require both partners to bind ligands for activation</p> Signup and view all the answers

    Why are Class I nuclear receptors crucial in embryogenesis and tissue development?

    <p>Maintenance of cellular homeostasis</p> Signup and view all the answers

    Which nuclear receptor is associated with cell growth reduction or increased susceptibility to apoptosis in prostate cancer cells?

    <p>RXRα</p> Signup and view all the answers

    Which type of nuclear receptors are involved in the modulation of cellular differentiation, development, and metabolism?

    <p>Class II/Type II</p> Signup and view all the answers

    Which drug is an AR antagonist used in the treatment of metastatic prostate cancer?

    <p>Flutamide</p> Signup and view all the answers

    What is the approved indication for Bexarotene, a RXR modulator?

    <p>CTCL treatment</p> Signup and view all the answers

    Which nuclear receptor drug is used for the treatment of non-metastatic CRPC?

    <p>Apalutamide</p> Signup and view all the answers

    Which nuclear receptor drug is known for its reduction in the risk of breast cancer?

    <p>Raloxifene</p> Signup and view all the answers

    Which class of nuclear receptors enhances peripheral insulin sensitivity and is used in Type II diabetes treatment?

    <p>Class II/Type II</p> Signup and view all the answers

    'Ligands of PPARα are clinically effective at lowering TG & LDL and increasing HDL' - This statement refers to the action of which type of drugs?

    <p>PPARα ligands</p> Signup and view all the answers

    Which nuclear receptor drug is used for the treatment of metastatic breast cancer and reducing the risk of breast cancer?

    <p>Tamoxifen</p> Signup and view all the answers

    What is the main function of nuclear receptors within the cell?

    <p>Transduce signals from lipophilic ligands to induce gene expression changes</p> Signup and view all the answers

    How many members are there in the human nuclear receptor superfamily?

    <p>48 members</p> Signup and view all the answers

    Which class of nuclear receptors functions as endocrine receptors that bind to specific DNA elements as homo-dimers?

    <p>Class I (Steroid Receptors/Nuclear Hormone Receptors)</p> Signup and view all the answers

    What is the main role of Class II (RXR Heterodimers) nuclear receptors?

    <p>Binding to DNA elements as hetero-dimers with the retinoid X receptor (RXR)</p> Signup and view all the answers

    Which statement best describes the role of nuclear receptor signalling in health and disease?

    <p>Plays key roles in the pathology of cancer, cardiovascular &amp; endocrine diseases, and inflammation.</p> Signup and view all the answers

    Which domain of nuclear receptors harbors the ligand-binding site and modulates co-activator & co-repressor binding?

    <p>Ligand-binding (E) domain</p> Signup and view all the answers

    What does the hinge region of nuclear receptors primarily do?

    <p>Plays a role in receptor dimerization</p> Signup and view all the answers

    What role does the Retinoid X Receptor (RXR) play in the body?

    <p>The Retinoid X Receptor (RXR) plays a role in lipid metabolism, apoptosis, and the immune system.</p> Signup and view all the answers

    How is the Progesterone Receptor (PR) involved in the development of the body?

    <p>The Progesterone Receptor (PR) plays a critical role in the development of mammary glands and other female reproductive organs.</p> Signup and view all the answers

    What are the essential functions of the Androgen Receptor (AR) in the male body?

    <p>The Androgen Receptor (AR) is essential for male sexual differentiation, bone growth, muscle homeostasis, and development.</p> Signup and view all the answers

    How does dysregulation of the Oestrogen Receptor (ER) impact health?

    <p>Dysregulation of the Oestrogen Receptor (ER) is associated with breast cancer development and metastasis.</p> Signup and view all the answers

    What are the consequences of mutations, misfolding, or alteration of signaling pathways involving Nuclear Receptors?

    <p>Mutations, misfolding, or alteration of signaling pathways can lead to systemic organ dysfunction and disease, including inflammation, cancer, diabetes, cardiovascular disease, obesity, and reproductive disorders.</p> Signup and view all the answers

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