GHSR
Ghrelin was originally isolated from the stomach mucosa and functions as the ligand of the growth hormone secretagogue receptor (GHSR). Ghrelin functions to modulate hormone secretion, energy balance, gastric acid release, appetite, gastric motility, insulin secretion and the turnover of gastric and intestinal mucosa. The local production of ghrelin and GHSR has been observed in many tissues including the kidney, stomach, small intestine, large intestine, hypothalamus, pituitary gland, endocrine pancreas and placenta. Ghrelin induces cancer cell proliferation through the GHS-R/Ras/PI3K/Akt/mTOR axis. Furthermore, ghrelin also promots oral cancer proliferation via modulation of GLUT1 expression. Ghrelin promotes cell migration and invasion by GHSR/PI3K/Akt signaling pathway that the mechanism is proven to be blocked by the ghrelin receptor antagonist. Furthermore, ghrelin is reported to induce cell migration via regulating GHSR/CaMKII/AMPK/NF-κB signaling pathway. Ghrelin plays an important role in several key processes of cancer progression, including cell proliferation, migration and invasion, the role of ghrelin in promoting or inhibiting cancer progression is still unclear.
References
1.Lin TC, et al. Biochim Biophys Acta Rev Cancer. 2017;1868(1):51–57.
References
1.Lin TC, et al. Biochim Biophys Acta Rev Cancer. 2017;1868(1):51–57.
GPCR/G Protein
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GHSR
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Relamorelin
catalog no : M34692
cas no: 661472-41-9
Relamorelin(BIM28131, RM131) is a selective and potent ghrelin/growth hormone secretagogue receptor (GHSR) agonist with high affinity for GHS-1a receptor (Ki value is 0.42 ± 0.063 nM). -
YIL 781
catalog no : M33951
cas no: 875258-85-8
YIL 781 is a selective ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM), showing a weak affinity for kinesin receptors (K = 6 μM). -
NF-56-EJ40 hydrochloride
catalog no : M33038
cas no: 2728500-80-7
NF-56-EJ40 hydrochloride is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. -
JMV 2959 hydrochloride (925238-89-7 free base)
catalog no : M32974
cas no: 2448414-54-6
JMV 2959 hydrochloride (925238-89-7 free base) is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells. -
des-Gln14-Ghrelin (rat)
catalog no : M30687
cas no: 293735-04-3
An endogenous ligand for the ghrelin receptor (GHS-R1a), produced by alternative splicing of the rat ghrelin gene. Potently induces Ca2+ release in cells expressing ghrelin receptors (EC50 = 2.4 nM) and stimulates GH release in vivo.