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Uncovering the Activation Mechanism of Class B GPCRs with Intracellular Agonists

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Uncovering the Activation Mechanism of Class B GPCRs with Intracellular Agonists

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Questions and Answers

True or false: Class B G-protein-coupled receptors (GPCRs) are not important drug targets

False

True or false: Injectable peptide drugs targeting GLP1R and PTH1R have been developed

True

True or false: Orally available small-molecule drugs targeting GLP1R and PTH1R are currently available

False

True or false: The high-resolution structure of human PTH1R in complex with Gs and a small-molecule agonist, PCO371, was reported in the article

True Signup and view all the answers

True or false: The binding site of PCO371 on PTH1R is located at the extracellular interface

False Signup and view all the answers

What is the main focus of the article?

The main focus of the article is the activation of class B G-protein-coupled receptors (GPCRs) by a biased intracellular agonist. Signup and view all the answers

Which receptors are mentioned as important drug targets?

Glucagon-like peptide 1 receptor (GLP1R) and parathyroid hormone 1 receptor (PTH1R) are mentioned as important drug targets. Signup and view all the answers

What is the binding site of PCO371 on PTH1R?

The binding site of PCO371 on PTH1R is located at the cytoplasmic interface. Signup and view all the answers

What is the current status of orally available small-molecule drugs targeting GLP1R and PTH1R?

Orally available small-molecule drugs targeting GLP1R and PTH1R remain under development. Signup and view all the answers

What is the purpose of the reported high-resolution structure?

The purpose of the reported high-resolution structure is to reveal the unexpected binding mode of PCO371 on PTH1R with Gs. Signup and view all the answers