CRF Receptor Family Related Drug Discovery Products
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Long regarded as one of the body's main regulators of the stress response, corticotropin-releasing factor (CRF) is a 41 amino acid neuropeptide that mediates neuroendocrine, autonomic, and behavioral responses to environmental demands. The CRF1 receptor and CRF2 receptor, two genes encoding unique G-protein coupled CRF receptors, have been discovered. However, recent research on the CRF receptor subtypes and CRF receptor-specific ligands raises the possibility that this system regulates stress differently and that imbalances in receptor activation may result in the emergence of psychiatric diseases linked to stress.
Fig.1. CRF family of peptide hormones.1,2
To meet the needs of CRF receptor family drug discovery, Creative Biolabs can provide a wide variety of related assays and products:
Overview of CRF Receptor Family
There are two known genes that encode different G-protein coupled CRF receptors. The CRF1 receptor is mostly present in the pituitary, amygdala, hippocampus, cerebellum, and cortex; when it is activated, stress-related behavior is frequently increased. The behavioral stress response is increased when CRF is present because it preferentially binds to the CRF1 receptor. Mice lacking the CRF1 receptor exhibit less spontaneous motor activity and a lower reactivity to stressful stimuli. Our findings indicating CRF1 receptor activation promotes behavioral stress response suggest that the CRF1 receptor may be a crucial biological regulator of stress-related psychiatric illnesses.
The ventromedial hypothalamus, choroid plexus, and lateral septum are the major locations of the CRF2 receptor. The changes in feeding behavior are most strongly correlated with CRF2 receptor activation. When tested in the elevated plus maze, open field, and light-dark emergence tests, CRF2 receptor knockout mice exhibit an anxiety-like behavior. Rats with central CRF2 receptor antisense infusion exhibit a decrease in stress coping mechanisms and an anxiogenic-like reaction.
CRF Receptor Family Drug Discovery
The reported data provide convincing evidence that the CRF system, a key stress response regulator, plays a critical role in regulating elevated stress, which in turn may result in stress-related mental illnesses. Instead of just CRF activation, these behavioral alterations seem to be the outcome of an imbalance in CRF1 and CRF2 receptor activity. Given the binding profile of these neuropeptides, it appears that the elevations in CRF frequently seen during the stress reaction cause an over activation of the CRF1 receptor. The evidence supporting the anti-stress role of CRF2 receptor activation provides more credence to the theory that the CRF1 receptor coordinates the activational components of stress while the CRF2 receptor serves as a coping mechanism to counteract this effect. Consequently, it seems that there are two possible strategies for the creation of novel antidepressant drugs.
References
- Vuppaladhadiam, Lahari, et al. "Corticotropin-releasing factor family: a stress hormone-receptor system's emerging role in mediating sex-specific signaling." Cells 9.4 (2020): 839.
- Distributed under Open Access License CC BY 4.0, without modification.
