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Questions and Answers
What is the function of the transmembrane domain of membrane receptors?
What is the function of the transmembrane domain of membrane receptors?
- It binds the first messenger
- It responds to the first messenger by changing conformation
- It allows transducer function
- It connects the two components (correct)
How do agonists affect the receptor?
How do agonists affect the receptor?
- They bind specifically to the receptor
- They cause a conformational change in the receptor (correct)
- They inhibit the function of antagonists
- They do not lead to an intracellular signal
What determines binding specificity and affinity between ligands and receptors?
What determines binding specificity and affinity between ligands and receptors?
- The type of transducer activated
- The number of domains in the receptor
- The location of the receptor
- The extent of molecular complementarity (correct)
What does a given ligand binding to different types of receptors activate?
What does a given ligand binding to different types of receptors activate?
What is the role of the intracellular domain of membrane receptors?
What is the role of the intracellular domain of membrane receptors?
How do antagonists affect the receptor?
How do antagonists affect the receptor?
In what way may two receptors that bind different ligands signal within a single cell?
In what way may two receptors that bind different ligands signal within a single cell?
What activates different cell responses with a given ligand binding to different types of receptors?
What activates different cell responses with a given ligand binding to different types of receptors?
What are the extracellular signaling molecules called?
What are the extracellular signaling molecules called?
Which organelles are involved in GPCR signaling according to the text?
Which organelles are involved in GPCR signaling according to the text?
What is the main role of G protein-coupled receptors (GPCRs) in cell signaling?
What is the main role of G protein-coupled receptors (GPCRs) in cell signaling?
What is the effect of GPCR and transducer/effector localization mentioned in the text?
What is the effect of GPCR and transducer/effector localization mentioned in the text?
Which physiological responses are controlled by activation of signaling pathways as per the text?
Which physiological responses are controlled by activation of signaling pathways as per the text?
What does insulin primarily regulate based on the information provided in the text?
What does insulin primarily regulate based on the information provided in the text?
Which location do membrane-bound receptors primarily occupy according to the text?
Which location do membrane-bound receptors primarily occupy according to the text?
Why are signaling pathways targeted by drugs according to the text?
Why are signaling pathways targeted by drugs according to the text?
Which proteins promote GTP hydrolysis by the α-subunit of heterotrimeric G proteins?
Which proteins promote GTP hydrolysis by the α-subunit of heterotrimeric G proteins?
How many types of alpha Gα subunits are there?
How many types of alpha Gα subunits are there?
Which type of G protein is designated by the alpha chain αs?
Which type of G protein is designated by the alpha chain αs?
What is the effector for the alpha subunit designated as Gs?
What is the effector for the alpha subunit designated as Gs?
How many types of beta Gg subunits are there?
How many types of beta Gg subunits are there?
What can different combinations of G protein subunits form?
What can different combinations of G protein subunits form?
What do HA-TAG proteins form with respect to G protein subunits?
What do HA-TAG proteins form with respect to G protein subunits?
What type of proteins are RGS domain-containing proteins?
What type of proteins are RGS domain-containing proteins?
How many regulators of G-protein signaling (RGS) domain-containing proteins have been identified in humans?
How many regulators of G-protein signaling (RGS) domain-containing proteins have been identified in humans?
What is the function of Gi with respect to adenylate cyclase?
What is the function of Gi with respect to adenylate cyclase?
What is the main difference between the topology of class A and class B receptors?
What is the main difference between the topology of class A and class B receptors?
What marked the beginning of model peptides binding to GPCRs according to the text?
What marked the beginning of model peptides binding to GPCRs according to the text?
What was used as the basis for the construction of the receptor molecular model?
What was used as the basis for the construction of the receptor molecular model?
Which study served as the basis for electron cryomicroscopy, contributing to the understanding of GPCR structure?
Which study served as the basis for electron cryomicroscopy, contributing to the understanding of GPCR structure?
How many distinct GPCRs and ligand-receptor interactions were studied in the pioneering study mentioned in the text?
How many distinct GPCRs and ligand-receptor interactions were studied in the pioneering study mentioned in the text?
What was solved by Hollens et al. in 2013 and Wu et al. in 2014 in relation to GPCR structural biology?
What was solved by Hollens et al. in 2013 and Wu et al. in 2014 in relation to GPCR structural biology?
What was noted as serving as a basis for the construction of receptor molecular models according to the text?
What was noted as serving as a basis for the construction of receptor molecular models according to the text?
What was bound to an inhibitor, as per the information provided in the text?
What was bound to an inhibitor, as per the information provided in the text?
What was the year when the 3D structure of bRho in its inactive state was first revealed?
What was the year when the 3D structure of bRho in its inactive state was first revealed?
Which family of GPCRs comprises fifteen receptors in humans and is activated by small molecules such as amino acids?
Which family of GPCRs comprises fifteen receptors in humans and is activated by small molecules such as amino acids?
Which part of the GPCR is called the 'venus flytrap domain' and contains the entire ligand binding site?
Which part of the GPCR is called the 'venus flytrap domain' and contains the entire ligand binding site?
Which type of GPCR family includes receptors for neurotransmitters and is classified into rhodopsin and nonrhodopsin receptors?
Which type of GPCR family includes receptors for neurotransmitters and is classified into rhodopsin and nonrhodopsin receptors?
Which class of GPCR-ligand complexes presents diverse ligand-binding sites for small molecules such as amino acids?
Which class of GPCR-ligand complexes presents diverse ligand-binding sites for small molecules such as amino acids?
Which representative structure from Class B GPCR-ligand complexes is bound to negative allosteric modulators?
Which representative structure from Class B GPCR-ligand complexes is bound to negative allosteric modulators?
What is the PDB ID associated with the representative structure from Class B GPCR-ligand complexes, CRF1?
What is the PDB ID associated with the representative structure from Class B GPCR-ligand complexes, CRF1?
What marked the beginning of GPCR structural biology?
What marked the beginning of GPCR structural biology?
In what form do classic C receptors exist?
In what form do classic C receptors exist?
What changes the orientation of transmembrane domains 3, 4, 5, 6, and 7?
What changes the orientation of transmembrane domains 3, 4, 5, 6, and 7?
What served as the basis for the construction of the receptor molecular model in GPCR structural biology?
What served as the basis for the construction of the receptor molecular model in GPCR structural biology?
What remained challenging despite relentless efforts in GPCR structural biology?
What remained challenging despite relentless efforts in GPCR structural biology?
What was released in 2000, a decade after the pioneering study of the 2D structure for bovine rhodopsin?
What was released in 2000, a decade after the pioneering study of the 2D structure for bovine rhodopsin?
What was calculated from the solved 2D crystals of bRho using electron cryomicroscopy?
What was calculated from the solved 2D crystals of bRho using electron cryomicroscopy?
What enhances the interaction of ECDs and changes the orientation of transmembrane domains?
What enhances the interaction of ECDs and changes the orientation of transmembrane domains?
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Study Notes
Membrane Receptors
- The transmembrane domain of membrane receptors is responsible for anchoring the receptor in the membrane and transmitting signals across the membrane.
- Agonists bind to receptors, causing a conformational change that activates the receptor and triggers a response.
- Binding specificity and affinity between ligands and receptors are determined by the shape and chemical properties of the ligand and the binding site on the receptor.
Signaling Pathways
- A given ligand binding to different types of receptors can activate different responses in a cell.
- The intracellular domain of membrane receptors is responsible for transmitting the signal to the interior of the cell.
- Antagonists bind to receptors, blocking the binding of agonists and preventing the activation of the receptor.
G Protein-Coupled Receptors (GPCRs)
- GPCRs are a type of membrane receptor that play a crucial role in cell signaling.
- GPCRs have an extracellular ligand-binding domain, a transmembrane domain, and an intracellular domain that interacts with G proteins.
- G proteins are heterotrimeric proteins consisting of α, β, and γ subunits.
- The main role of GPCRs in cell signaling is to transmit signals from extracellular ligands to intracellular effectors.
G Protein Signaling
- GPCR signaling involves the activation of G proteins, which in turn activate downstream effectors.
- The localization of GPCRs and transducers/effectors can affect the signaling pathway.
- Physiological responses controlled by activation of signaling pathways include vision, smell, taste, and hormone regulation.
- Insulin primarily regulates glucose metabolism.
G Protein Subunits
- There are several types of alpha Gα subunits, including Gαs, Gαi, and Gαq.
- The alpha subunit designated as Gs activates adenylate cyclase.
- There are several types of beta Gβ subunits.
- Different combinations of G protein subunits can form, leading to diverse signaling pathways.
Regulators of G-Protein Signaling (RGS)
- RGS proteins are negative regulators of G protein signaling.
- RGS domain-containing proteins promote GTP hydrolysis by the α-subunit of heterotrimeric G proteins.
- There are several RGS proteins identified in humans.
GPCR Structure
- The topology of class A and class B receptors differs, with class A having a more compact structure.
- The 3D structure of bRho in its inactive state was first revealed in 2000.
- The "venus flytrap domain" is the part of the GPCR that contains the entire ligand binding site.
GPCR Families
- The family of GPCRs that comprises fifteen receptors in humans and is activated by small molecules such as amino acids is the glutamate receptor family.
- The GPCR family that includes receptors for neurotransmitters and is classified into rhodopsin and nonrhodopsin receptors is the Class A GPCR family.
- The class of GPCR-ligand complexes that presents diverse ligand-binding sites for small molecules such as amino acids is the Class B GPCR family.
GPCR-Ligand Complexes
- The representative structure from Class B GPCR-ligand complexes is bound to negative allosteric modulators.
- The PDB ID associated with the representative structure from Class B GPCR-ligand complexes, CRF1, is 4KVM.
GPCR Structural Biology
- The pioneering study of the 2D structure for bovine rhodopsin marked the beginning of GPCR structural biology.
- The 3D structure of GPCRs remained challenging to determine despite relentless efforts.
- Electron cryomicroscopy was used to study the structure of GPCRs.
- HA-TAG proteins form complexes with G protein subunits.
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