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) (B)</p> Signup and view all the answers

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

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

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

<p>Cancer progression (A)</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 (A)</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 (D)</p> Signup and view all the answers

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

<p>TR-RXR (C)</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 (A)</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 (B)</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 (D)</p> Signup and view all the answers

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

<p>Maintenance of cellular homeostasis (D)</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 (B)</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 (D)</p> Signup and view all the answers

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

<p>Flutamide (A)</p> Signup and view all the answers

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

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

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

<p>Apalutamide (A)</p> Signup and view all the answers

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

<p>Raloxifene (A)</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 (C)</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 (B)</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 (B)</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 (D)</p> Signup and view all the answers

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

<p>48 members (C)</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) (D)</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) (A)</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. (A)</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 (B)</p> Signup and view all the answers

What does the hinge region of nuclear receptors primarily do?

<p>Plays a role in receptor dimerization (C)</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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