35 Questions
What can lead to systemic organ dysfunction and disease, including inflammation, cancer, diabetes, cardiovascular disease, obesity, and reproductive disorders?
Mutations, misfolding, or alteration of signaling pathways
Which nuclear receptor is essential for male sexual differentiation, bone growth, muscle homeostasis, and development?
Androgen Receptor (AR)
What role does the Progesterone Receptor (PR) play in the body?
Development of mammary glands & other female reproductive organs
Which nuclear receptor is associated with breast cancer development & metastasis when dysregulated?
Oestrogen Receptor (ER)
What functions are promoted by downregulation or loss of RXR signaling?
Inflammation of vital organ systems
Which nuclear receptor plays a key role in lipid metabolism, apoptosis, and the immune system?
Retinoid X Receptors (RXRs)
What is a common consequence of dysregulation of nuclear receptor signaling in the body?
Cancer progression
What is the initial event in the activation of Class I nuclear receptors?
Binding of steroid hormone
What is the final step in the activation pathway of Class I nuclear receptors?
Binding to hormone response elements on DNA
Which subclassification of nuclear receptors generally requires ligand binding for both partners to activate?
TR-RXR
What is the role of co-repressor complexes like NCoR and SMRT in Class II nuclear receptor signaling?
Confer ligand-independent repression when bound to heterodimers
Which nuclear receptor superfamily plays a significant role in lipid metabolism and inflammatory signaling?
Class II NRs
How do Class II nuclear receptors like PPAR-RXR and LXR-RXR differ in their ligand binding requirements?
'Permissive' complexes require both partners to bind ligands for activation
Why are Class I nuclear receptors crucial in embryogenesis and tissue development?
Maintenance of cellular homeostasis
Which nuclear receptor is associated with cell growth reduction or increased susceptibility to apoptosis in prostate cancer cells?
RXRα
Which type of nuclear receptors are involved in the modulation of cellular differentiation, development, and metabolism?
Class II/Type II
Which drug is an AR antagonist used in the treatment of metastatic prostate cancer?
Flutamide
What is the approved indication for Bexarotene, a RXR modulator?
CTCL treatment
Which nuclear receptor drug is used for the treatment of non-metastatic CRPC?
Apalutamide
Which nuclear receptor drug is known for its reduction in the risk of breast cancer?
Raloxifene
Which class of nuclear receptors enhances peripheral insulin sensitivity and is used in Type II diabetes treatment?
Class II/Type II
'Ligands of PPARα are clinically effective at lowering TG & LDL and increasing HDL' - This statement refers to the action of which type of drugs?
PPARα ligands
Which nuclear receptor drug is used for the treatment of metastatic breast cancer and reducing the risk of breast cancer?
Tamoxifen
What is the main function of nuclear receptors within the cell?
Transduce signals from lipophilic ligands to induce gene expression changes
How many members are there in the human nuclear receptor superfamily?
48 members
Which class of nuclear receptors functions as endocrine receptors that bind to specific DNA elements as homo-dimers?
Class I (Steroid Receptors/Nuclear Hormone Receptors)
What is the main role of Class II (RXR Heterodimers) nuclear receptors?
Binding to DNA elements as hetero-dimers with the retinoid X receptor (RXR)
Which statement best describes the role of nuclear receptor signalling in health and disease?
Plays key roles in the pathology of cancer, cardiovascular & endocrine diseases, and inflammation.
Which domain of nuclear receptors harbors the ligand-binding site and modulates co-activator & co-repressor binding?
Ligand-binding (E) domain
What does the hinge region of nuclear receptors primarily do?
Plays a role in receptor dimerization
What role does the Retinoid X Receptor (RXR) play in the body?
The Retinoid X Receptor (RXR) plays a role in lipid metabolism, apoptosis, and the immune system.
How is the Progesterone Receptor (PR) involved in the development of the body?
The Progesterone Receptor (PR) plays a critical role in the development of mammary glands and other female reproductive organs.
What are the essential functions of the Androgen Receptor (AR) in the male body?
The Androgen Receptor (AR) is essential for male sexual differentiation, bone growth, muscle homeostasis, and development.
How does dysregulation of the Oestrogen Receptor (ER) impact health?
Dysregulation of the Oestrogen Receptor (ER) is associated with breast cancer development and metastasis.
What are the consequences of mutations, misfolding, or alteration of signaling pathways involving Nuclear Receptors?
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.
Learn about the different major receptor superfamily types and their common characteristics in the MPharm PHA112 course. This quiz covers the basic molecular structures and signal transduction pathways of ligand-gated, G-protein-coupled, and kinase-linked receptors.
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