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Human ghrelin receptor (GHSR) is a recognized prospective target in the diagnosis and therapy of multiple cancer types. To gain a better understanding of this receptor signaling system, we have synthesized a novel full-length ghrelin analog that is fluorescently labeled at the side-chain of a C-terminal cysteine extension. This analog exhibited nanomolar affinity and potency for the ghrelin receptor. It shows comparable efficacy with that of endogenous ghrelin. The fluorescently-labeled ghrelin analog is a valuable tool for in vitro imaging of cell lines that express ghrelin receptor.
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http://dx.doi.org/10.1016/j.bbrc.2020.09.028 | DOI Listing |
Cell Rep
September 2025
Center for Hypothalamic Research, Department of Internal Medicine, UT Southwestern Medical Center, Dallas, TX, USA; Peter O'Donnell Jr. Brain Institute, UT Southwestern Medical Center, Dallas, TX, USA; Division of Endocrinology & Metabolism, Department of Internal Medicine, UT Southwestern Medical C
Food consumption impacts body weight differently depending on the time of day. Here, we investigated whether suprachiasmatic nucleus (SCN) neurons responsive to the hormone ghrelin temporally regulate eating and body weight in mice. The chemogenetic stimulation of GHSR (growth hormone secretagogue receptor)-expressing SCN neurons during the mid-rest phase-when mice are most sensitive to ghrelin's orexigenic effects-increased food intake.
View Article and Find Full Text PDFNutrients
August 2025
College of Food Science, South China Agriculture University, Guangzhou 510642, China.
Type 2 diabetes (T2D) is a complex metabolic disease characterized by chronic hyperglycemia due to insulin resistance and inadequate insulin secretion. Beyond the classically implicated organs, emerging evidence highlights the gut as a central player in T2D pathophysiology through its interactions with metabolic organs. The gut hosts trillions of microbes and enteroendocrine cells that influence inflammation, energy homeostasis, and hormone regulation.
View Article and Find Full Text PDFMedicina (Kaunas)
August 2025
Department of Nutrition and Dietetics, Faculty of Health Sciences, Hacettepe University, 06100 Ankara, Turkey.
: Ghrelin plays key roles in appetite regulation, involving both homeostatic and hedonic pathways. In obesity, its metabolism is affected by alterations in neural and hormonal responses. Liver-Enriched Antimicrobial Peptide 2 (LEAP2), recently identified as an endogenous ghrelin receptor antagonist, has emerged as a potential regulator of appetite and energy balance, and bariatric surgery is known to induce changes in this system.
View Article and Find Full Text PDFJ Cell Physiol
August 2025
Department of Physiology, School of Medicine, Jinan University, Guangzhou, China.
Ghrelin is a peptide hormone primarily produced by ghrelin cells in the stomach, playing a vital role in the regulation of eating behavior. Adenyl cyclase 8 (ADCY8), a key downstream signaling factor of G protein-coupled receptors, is essential for maintaining energy homeostasis by modulating levels of cyclic adenosine monophosphate (cAMP). Nevertheless, how ADCY8 modulates ghrelin levels and affects food intake is not well understood.
View Article and Find Full Text PDFSci Rep
August 2025
Department of Rehabilitation Medicine of Korean Medicine, Dongguk University, 814 Siksa-dong, Ilsandong-gu, Goyang-si, 10326, Republic of Korea.
Dyspepsia is a prevalent refractory condition that arises from various causes and lacks definitive treatment. There is an urgent need for evidence to support the use of herbal medicines in the treatment of gastroenterological disorders. This study aimed to compare the therapeutic effects of two common herbal formulas-namely, Shihosogan-tang (SST) and Yijung-tang (YJT)-on loperamide (LOP)-induced dyspepsia and to explore their potential mechanisms.
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