Table 1.
Examples of GPCRs in the pancreatic islet for receiving circulatory inputs.
GPCR | Family | Ligands | Transduction mechanism | Functions | References |
---|---|---|---|---|---|
GHSR1a | Rhodopsin | Ghrelin | Gq/11; Gi/o; G12/13 |
• Inhibit insulin secretionb | (12) |
GPR40 | Rhodopsin | Long-chain carboxylic acid | Gq/11; Gs; Gi/o |
• Stimulate glucagon secretionc • Enhance insulin secretiona |
(13, 14) |
GPR119 | Rhodopsin | N-oleoylethanolamide | Gs | • Enhance insulin secretionc • Stimulate β-cell replicationc |
(15, 16) |
ChemR23 | Rhodopsin | Chemerin | Gi/o | • Stimulate glucagon secretionc • Enhance insulin secretiona |
(17) |
MT1 | Rhodopsin | Melatonin | Gi/o; Gq/11 |
• Stimulate glucagon secretiona • Enhance insulin secretionb |
(18) |
MT2 | Rhodopsin | Melatonin | Gi/o | • Stimulate glucagon secretiona • Enhance insulin secretionb |
(18) |
α2AAR | Rhodopsin | Adrenaline; Noradrenaline | Gi/o; Gs |
• Inhibit insulin secretionb | (19) |
β1AR | Rhodopsin | Adrenaline; Noradrenaline | Gs; Gi/o; β-arrestin |
• Stimulate glucagon secretiona • Stimulate somatostatin secretiona |
(19, 20) |
β2AR | Rhodopsin | Adrenaline; Noradrenaline | Gs; Gi/o; β-arrestin 1 |
• Stimulate glucagon secretiona • Stimulate somatostatin secretiona |
(19, 20) |
β3AR | Rhodopsin | Adrenaline; Noradrenaline | Gs; Gi/o |
• Enhance insulin secretionb | (21) |
PAC1 | Secretin | PACAP | Gs; Gq/11 | • Enhance insulin secretionb • Stimulate glucagon secretiona |
(22, 23) |
GLP1R | Secretin | GLP1 | Gs | • Inhibit cytokine-induced apoptosis of β-cellsc • Inhibit glucagon secretionb |
(14) |
GIPR | Secretin | GIP | Gs | • Inhibit cytokine-induced apoptosisc • Induce insulin production regulated by inflammationb |
(14, 24) |
The GCPRs expressed in the pancreatic islet receive circulatory signals and exert their functions on hormone-secreting cells, initiating the autocrine and/or paracrine regulations between pancreatic cells. The primary transduction mechanisms are listed at the first row followed by secondary transduction mechanisms (if any).
Initiate both autocrine and paracrine regulations.
Initiate paracrine regulations.
Initiate autocrine regulations.