Ghrelin receptor signaling: a promising therapeutic target for metabolic syndrome and cognitive dysfunction.
The neuroendocrine hormone ghrelin is an octanoylated 28-residue peptide that exerts numerous physiological functions. Ghrelin exerts its effects on the body mainly through a highly conserved G protein-coupled receptor known as the growth hormone secretagagogue receptor subtype 1a (GHS-R1a). Ghrelin and GSH-R1a are widely expressed in both peripheral and central tissues/organs, and ghrelin signaling plays a critical role in maintaining energy balance and neuronal health. The multiple orexigenic effects of ghrelin and its receptor have been studied in great detail, and GHS-R1a-mediated ghrelin signaling has long been a promising target for the treatment of metabolic disorders, such as obesity. In addition to its well-characterized metabolic effects, there is also mounting evidence that ghrelin-mediated GHS-R1a signaling exerts neuroprotective effects on the brain. In this review, we will summarize some of the effects of ghrelin-mediated GSH-R1a signaling on peripheral energy balance and cognitive function. We will also discuss the potential pharmacotherapeutic role of GSH-R1a-mediated ghrelin signaling for the treatment of complex neuroendocrine disorders.
Cong
Wei-na
WN
Metabolism Unit, Laboratory of Clinical Investigation, National Institute on Aging, Baltimore, MD 21224, USA.
Golden
Erin
E
Pantaleo
Nick
N
White
Caitlin M
CM
Maudsley
Stuart
S
Martin
Bronwen
B
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism / Q000502:physiology; D003072:Cognition Disorders / Q000188:drug therapy*; D016503:Drug Delivery Systems / Q000379:methods*; D004734:Energy Metabolism / Q000502:physiology; D054439:Ghrelin / Q000378:metabolism / Q000502:physiology; D006801:Humans; D024821:Metabolic Syndrome / Q000188:drug therapy*; D008954:Models, Biological; D054440:Receptors, Ghrelin / Q000187:drug effects* / Q000502:physiology; D015398:Signal Transduction / Q000187:drug effects* / Q000502:physiology
D054439:Ghrelin; D054440:Receptors, Ghrelin