Cortistatins
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Introduction
In 1996, de Lecea et al found a new neuroendocrine polypeptide that inhibits cortical activity in the mammalian cerebral cortex, named cortistatins. Cortistatin is a new member of the somatostatin family and has a structure similar to somatostatin (SST)). Cortistatins bind to its receptors and exhibit diverse biological activities. They can regulate the physiological functions of the nervous system, immune system and endocrine system. They have neuromodulation effects such as inhibition of exercise, induction of sleep, affecting learning and memory, and certain neuroprotective effects. Moreover, cortistatins are involved in regulating the release of immune and endocrine hormones, maintaining the homeostasis of the body's environment.
Mechanism of action
Cortistatins are capable of binding to three receptors: somatostatin receptors (SSTR), growth hormone secretagogues receptor 1a (GHSR1a), and mas-related gene 2 receptor (MrgX2). It was found that Cortistatins-14 and Cortistatins-17 bind to radiolabeled SST-14 with high affinity and bind to SSTR1-5 cells of transfected SSTR1-5 cells and normal human thymic tissue cells. Cortistatins-14 has also been shown to be effective in activating SSTR on GH4 cells. MrgX2 is a receptor that selectively binds to cortistatins, first discovered in vivo by Robas et al in 2003. Cortistatins selectively bind to MrgX2 and may be involved in the regulation of pain perception, but the results also indicate whether MrgX2 is a specific receptor for cortistatins.
Application of Cortistatins
The high expression of cortistatins is present in the body's immune tissues, indicating that cortistatins are involved in immune regulation in vivo. During animal endotoxemia, cortistatins prevent the invasion of inflammatory cells and the intravascular coagulation of multiple organs. These studies have shown that cortistatins are involved in the regulation of inflammation and are a promising multi-level anti-inflammatory drug.
Reference
- de Lecea, L., et al. (1996) A cortical neuropeptide with neuronal depressant and sleep modulating properties. Nature, 381(6579): 242-245.
