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| Figure 10: Binding Models of Orthosteric and Allosteric Agonists of Class B GPCRs. (A) The general peptide (orthosteric) binding model for class B GPCRs is shown. The C-terminal region of the orthosteric peptide binds to the N-terminal region of the GPCR. This results in a weak interaction and consequently causes the formation of a bi-tethered confirmation. (B) Non-peptide (allosteric) binding and antagonist model for class GPCRs. Non-peptide/ antagonist (blue circle) binds the receptor and causes a conformational change that prevents peptide binding. This non-peptide interaction can either block peptide stimulated receptor signaling or may not affect peptide binding to the N-terminal domain of the GPCR. |
