Podcast
Questions and Answers
What is the structure of a GPCR?
What is the structure of a GPCR?
- 4 transmembrane protein with N term in extracellular part and C term in intracellular
- 5 transmembrane protein with N term in intracellular part and C term in extracellular
- 6 transmembrane protein with N term in intracellular part and C term in extracellular
- 7 transmembrane protein with N term in extracellular part and C term in intracellular (correct)
How many receptors within the GPCR SuperFamily have unknown function?
How many receptors within the GPCR SuperFamily have unknown function?
- More than 800
- More than 1000
- More than 400
- More than 600 (correct)
What happens to GDP when a heterotrimeric G protein is activated?
What happens to GDP when a heterotrimeric G protein is activated?
- It hydrolyzes to GTP (correct)
- It is phosphorylated
- It remains unchanged
- It dissociates from the alpha subunit
What are the modes of internalization for GPCRs?
What are the modes of internalization for GPCRs?
Which part of the Golgi Apparatus receives newly synthesized proteins?
Which part of the Golgi Apparatus receives newly synthesized proteins?
What are RAMPs in relation to GPCRs?
What are RAMPs in relation to GPCRs?
What are the types of signaling initiation for GPCRs?
What are the types of signaling initiation for GPCRs?
Which domain of a GPCR constitutes the transmembrane portion?
Which domain of a GPCR constitutes the transmembrane portion?
What are the subunits of a heterotrimeric G protein?
What are the subunits of a heterotrimeric G protein?
What are the methods of exiting Trans-Golgi Network (TGN)?
What are the methods of exiting Trans-Golgi Network (TGN)?
Which type of vesicles have many similarities to GSVs and are located in the pituitary gland to regulate the activity of the adrenal gland?
Which type of vesicles have many similarities to GSVs and are located in the pituitary gland to regulate the activity of the adrenal gland?
Which type of somatostatin receptors are internalized very quickly and recycle slowly?
Which type of somatostatin receptors are internalized very quickly and recycle slowly?
What is the pH range along the endocytotic pathway that allows lysosomes to degrade better and receptors to be separated from their ligands?
What is the pH range along the endocytotic pathway that allows lysosomes to degrade better and receptors to be separated from their ligands?
Which type of GPCR receptor has low affinity for visual arrestin and does not co-localize in endosomes?
Which type of GPCR receptor has low affinity for visual arrestin and does not co-localize in endosomes?
What is the post-endocytic trafficking pathway of sst2A somatostatin receptors?
What is the post-endocytic trafficking pathway of sst2A somatostatin receptors?
What is the effect of Brefeldin A on SSTR2 and syntaxin-6?
What is the effect of Brefeldin A on SSTR2 and syntaxin-6?
What happens when Class A GPCR receptors undergo ubiquitination?
What happens when Class A GPCR receptors undergo ubiquitination?
What is the system that allows cells to adapt to environmental changes such as those in adipose tissue, muscle, and liver?
What is the system that allows cells to adapt to environmental changes such as those in adipose tissue, muscle, and liver?
What is the location of GSVLs?
What is the location of GSVLs?
Which type of GPCR receptor has high affinity for visual arrestin and co-localizes in endosomes?
Which type of GPCR receptor has high affinity for visual arrestin and co-localizes in endosomes?
Which RAMP binds to CLR, making it the receptor for AM1, a protein hormone with vasodilator effects?
Which RAMP binds to CLR, making it the receptor for AM1, a protein hormone with vasodilator effects?
What is the receptor for CGRP, a neuropeptide modulating pain transmission?
What is the receptor for CGRP, a neuropeptide modulating pain transmission?
Which type of receptors require both wildtype isoforms for a functioning receptor at the cell surface?
Which type of receptors require both wildtype isoforms for a functioning receptor at the cell surface?
How many groups of GRKs play a role in GPCR desensitization?
How many groups of GRKs play a role in GPCR desensitization?
What type of desensitization involves direct phosphorylation by GRK2, specific to the receptor?
What type of desensitization involves direct phosphorylation by GRK2, specific to the receptor?
Which type of receptors prefer homologous desensitization due to more sites for GRK phosphorylation?
Which type of receptors prefer homologous desensitization due to more sites for GRK phosphorylation?
What is the structure of a GPCR?
What is the structure of a GPCR?
How many receptors within the GPCR SuperFamily have unknown function?
How many receptors within the GPCR SuperFamily have unknown function?
What are the modes of internalization for GPCRs?
What are the modes of internalization for GPCRs?
What is the effect of Brefeldin A on GPCR trafficking?
What is the effect of Brefeldin A on GPCR trafficking?
What are RAMPs in relation to GPCRs?
What are RAMPs in relation to GPCRs?
What is the role of Heterotrimeric G Proteins when activated?
What is the role of Heterotrimeric G Proteins when activated?
Which domain of a GPCR constitutes the transmembrane portion?
Which domain of a GPCR constitutes the transmembrane portion?
What are the parts of Golgi Apparatus in sequence from receiving newly synthesized proteins to sending them to the plasma membrane?
What are the parts of Golgi Apparatus in sequence from receiving newly synthesized proteins to sending them to the plasma membrane?
What are the types of signaling initiation for GPCRs?
What are the types of signaling initiation for GPCRs?
Which type of receptors require both wildtype isoforms for a functioning receptor at the cell surface?
Which type of receptors require both wildtype isoforms for a functioning receptor at the cell surface?
Which GPCR-associated protein has four functions including chaperone, pharmacology switch, signaling switch, and trafficking switch?
Which GPCR-associated protein has four functions including chaperone, pharmacology switch, signaling switch, and trafficking switch?
Which GPCR receptor is closely related to the calcitonin receptor (CTP) and interacts with RAMPs?
Which GPCR receptor is closely related to the calcitonin receptor (CTP) and interacts with RAMPs?
Which GPCR-associated protein is brought to the receptor by arrestin and stops GPCR signaling?
Which GPCR-associated protein is brought to the receptor by arrestin and stops GPCR signaling?
Which type of GPCR desensitization involves four steps and three groups of GRKs?
Which type of GPCR desensitization involves four steps and three groups of GRKs?
Which type of somatostatin receptors exhibit different internalization and externalization responses?
Which type of somatostatin receptors exhibit different internalization and externalization responses?
What is the widespread location of GABAB receptor in the body?
What is the widespread location of GABAB receptor in the body?
What are the two isoforms of the GABAB receptor?
What are the two isoforms of the GABAB receptor?
What are the two functions of arrestins in relation to GPCR desensitization?
What are the two functions of arrestins in relation to GPCR desensitization?
What is the enzyme that stops GPCR signaling by interacting with arrestin?
What is the enzyme that stops GPCR signaling by interacting with arrestin?
What structure causes invaginations of the plasma membrane and is involved in GPCR internalization?
What structure causes invaginations of the plasma membrane and is involved in GPCR internalization?
What is the pH range along the endocytotic pathway that allows lysosomes to degrade better and receptors to be separated from their ligands?
What is the pH range along the endocytotic pathway that allows lysosomes to degrade better and receptors to be separated from their ligands?
Which type of GPCR receptor has low affinity for visual arrestin and does not co-localize in endosomes?
Which type of GPCR receptor has low affinity for visual arrestin and does not co-localize in endosomes?
What is the post-endocytic trafficking pathway of sst2A somatostatin receptors?
What is the post-endocytic trafficking pathway of sst2A somatostatin receptors?
What happens when Class A GPCR receptors undergo ubiquitination?
What happens when Class A GPCR receptors undergo ubiquitination?
What are GSVLs and where are they located?
What are GSVLs and where are they located?
Which type of somatostatin receptors are internalized very quickly and recycle slowly?
Which type of somatostatin receptors are internalized very quickly and recycle slowly?
What is the system that allows cells to adapt to environmental changes such as those in adipose tissue, muscle, and liver?
What is the system that allows cells to adapt to environmental changes such as those in adipose tissue, muscle, and liver?
Which type of GPCR receptor has high affinity for visual arrestin and co-localizes in endosomes?
Which type of GPCR receptor has high affinity for visual arrestin and co-localizes in endosomes?
What happens to GDP when a heterotrimeric G protein is activated?
What happens to GDP when a heterotrimeric G protein is activated?
What is the effect of Brefeldin A on SSTR2 and syntaxin-6?
What is the effect of Brefeldin A on SSTR2 and syntaxin-6?
Flashcards
What are RAMPs?
What are RAMPs?
RAMPs are a family of proteins that interact with G protein-coupled receptors (GPCRs) and influence their function.
How are RAMPs related?
How are RAMPs related?
RAMP1 and RAMP3 are more closely related to each other than to RAMP2.
What are the key functions of RAMPs?
What are the key functions of RAMPs?
RAMPs act as chaperones, pharmacology switches, signaling switches, and trafficking switches for GPCRs.
What is the calcitonin receptor?
What is the calcitonin receptor?
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What is CLR?
What is CLR?
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What happens when CLR binds to RAMP1?
What happens when CLR binds to RAMP1?
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What happens when CLR binds to RAMP2?
What happens when CLR binds to RAMP2?
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What happens when CLR binds to RAMP3?
What happens when CLR binds to RAMP3?
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What are GABAB receptors?
What are GABAB receptors?
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What is a unique requirement of GABAB receptors?
What is a unique requirement of GABAB receptors?
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What is GPCR desensitization?
What is GPCR desensitization?
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What are the steps involved in GPCR desensitization?
What are the steps involved in GPCR desensitization?
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What are GRKs?
What are GRKs?
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How are GRKs categorized?
How are GRKs categorized?
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What is homologous desensitization?
What is homologous desensitization?
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What is heterologous desensitization?
What is heterologous desensitization?
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Why do beta2 adrenergic receptors prefer homologous desensitization?
Why do beta2 adrenergic receptors prefer homologous desensitization?
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What are arrestins?
What are arrestins?
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How many types of arrestins are there?
How many types of arrestins are there?
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What are the functions of arrestins?
What are the functions of arrestins?
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What is PDE4?
What is PDE4?
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What are caveolae?
What are caveolae?
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Study Notes
Evolution and Functions of GPCRs and RAMPs
- RAMPs are highly conserved, with RAMP1 and RAMP3 being more closely related than RAMP2.
- RAMPs serve as chaperones, pharmacology switches, signaling switches, and trafficking switches for GPCRs.
- The calcitonin receptor (CTP) interacts with RAMPs and is closely related to CLR (calcitonin-like receptor).
- CLR binds to RAMP1 and becomes the receptor for CGRP, a neuropeptide modulating pain transmission.
- RAMP2 binds to CLR, making it the receptor for AM1, a protein hormone with vasodilator effects.
- RAMP3 binds to CLR, making it the receptor for AM2, a hormone regulating glucose levels.
- GABAB receptors, mediating rapid action ion channels, require both wildtype isoforms for a functioning receptor at the cell surface.
- GPCR desensitization involves a 4-step process: resting state, stimulation, phosphorylation, and desensitization.
- Three groups of GRKs play a role in GPCR desensitization, with different locations and domains.
- Homologous desensitization involves direct phosphorylation by GRK2, specific to the receptor, while heterologous desensitization involves second messenger kinases.
- Beta2 adrenergic receptors prefer homologous desensitization due to more sites for GRK phosphorylation.
- Arrestins are key adaptor proteins in GPCR desensitization and internalization, with four types and specific functions in stopping signaling and binding to GPCR.
Functions and Mechanisms of GPCR-Associated Proteins
- RAMPs, highly conserved, with RAMP1 and RAMP3 more closely related than RAMP2
- Four functions of RAMP: chaperone, pharmacology switch, signaling switch, trafficking switch
- Calcitonin receptor (CTP) interacts with RAMPs, closely related to CLR (calcitonin-like receptor)
- GABAB receptor, widespread in CNS, has two isoforms and a quality control mechanism
- sst2A and sst5, somatostatin receptors, exhibit different internalization and externalization responses
- Betanergic (B1) receptors extensively studied and used as GPCR model
- GPCR desensitization involves four steps and three groups of GRKs
- Homologous and heterologous desensitization of GPCRs, with beta2 adrenergic receptors preferring homologous desensitization
- Arrestins, key adaptor proteins in GPCR desensitization and internalization, have four types
- Arrestins have two functions: stopping signaling by binding to GPCR and direct binding to clathrin-coated pits
- PDE4, an enzyme brought to the receptor by arrestin, stops GPCR signaling
- Caveolae, formed by myelin, cause invaginations of the plasma membrane and are involved in GPCR internalization
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Description
Test your knowledge of G protein-coupled receptors (GPCRs) and heterotrimeric G proteins. Learn about the structure of GPCRs, the GPCR superfamily, hydrophobic and hydrophilic domains, and the types of signaling initiation. Explore the composition and activation of heterotrimeric G proteins.
