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Comment
. 2017 Jun 1;158(6):1560-1563.
doi: 10.1210/en.2017-00252.

Incretin-Based Therapies: Revisiting Their Mode of Action

Brian T Layden  1   2 , Barton Wicksteed  1 , Franck Mauvais-Jarvis  3
Affiliations
Comment

Incretin-Based Therapies: Revisiting Their Mode of Action

Brian T Layden et al. Endocrinology. .
No abstract available

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Figures

Figure 1.
Figure 1.
GPCR signaling events that may be differentially contributing to aspects of β-cell function and proliferation. (1) GPCR activation leads to Gα downstream signaling effects that mediate aspects of β-cell function and proliferation. (2) Gβγ may also influence β-cell function and proliferation. (3) Evidence suggests that β-arrestin (β-Ar) mediates β-cell function/proliferation. (4) When GPCRs are activated, each receptor (R) is internalized, recycled, or degraded at differential rates. (5) GPCRs can form dimers (homodimers or heterodimers) in which each of these five steps can influence receptor signaling abilities. (A) Receptor internalization can result in rapid return to the plasma membrane or a more profound downregulation, influencing the GPCR’s signaling abilities. (B) β-arrestin, which contributes to the downregulation process, also can activate pathways such as ERK. Zhu et al. (19)demonstrated the importance of β-arrestin in β-cell function. (C) Gα proteins, in particular Gsα, Gq/11α, or Gi/oα, and downstream signals, influencing β-cell function. Multiple other G-protein modulators influence the inactivation of Gα proteins. (D) Gβγ can influence ion channel function, mitogen-activated protein kinases activation, and adenylate cyclase properties, among others.
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