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
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
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Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
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Other Targets(3)
OXTR(2)
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PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
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GHSR
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Relamorelin
产品货号 : M34692
cas no: 661472-41-9
Relamorelin (RM-131),一种生长素类似物,是一种选择性的生长素释放肽/生长激素促分泌素受体 (GHSR) 激动剂,对 GHS-1a 受体的 Ki 值为 0.42 nM。Relamorelin 是一种五肽,具有中枢渗透性。Relamorelin 增加生长激素水平,加速胃排空,具有用于恶病质、胃轻瘫和胃/肠运动障碍研究的潜力。 -
YIL 781
产品货号 : M33951
cas no: 875258-85-8
YIL781 是有效的、具有口服活性的胃促生长素受体(GHSR) 的拮抗剂。YIL781 可改善大鼠体内葡萄糖稳态。YIL781 可抑制饥饿素诱导的钙反应,pIC50 值分别为 7.90 和 8.27。 -
NF-56-EJ40 hydrochloride
产品货号 : 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. NF-56-EJ40 hydrochloride has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM. -
JMV 2959 hydrochloride (925238-89-7 free base)
产品货号 : M32974
cas no: 2448414-54-6
JMV 2959 hydrochloride 是一种生长激素促分泌素受体 1a 型 (GHS-R1a) 拮抗剂,作用于 LLC-PK1 细胞,抑制 GHS-R1a,IC50 值为 32±3 nM。 -
des-Gln14-Ghrelin (rat)
产品货号 : 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.