Enkephalins and Proenkephalins

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Introduction

Enkephalin (ENK) was first discovered by Hughes in 1975. It belongs to endogenous opioids and is widely distributed in the body. It binds to different types of opioid receptors and exerts various biological regulation effects. Studies have shown that enkephalin comprises two pentapeptides, Methionine enkephalin (MEK) and Leucine enkephalin (LEK), which are derived from the same precursor, proenkephalin. Effective activation of endogenous ENK allows its physiological function to be fully utilized to induce effective analgesia and enhance immune function.

Mechanism of action

ENK binds to endogenous opioid peptide receptors, and endogenous opioid peptide receptors are classified into μ, δ, κ, etc. while ENK mainly acts on δ-type receptors. The receptors are mainly located in the central nervous system and regulate the pain-related anatomical sites, which are also the areas with the highest concentration of immunoreactive ENK. ENK regulates the secretion of prolactin, thyrotropin, and growth hormone. From the structure of the ENK distribution in the edge system, it is suggested that ENK is related to emotional response. In particular, LEK has strong binding to δ receptors, and δ receptors may be involved in emotional regulation activities such as euphoria and reward behavior. Under certain conditions, MENK binds to the κ and δ receptors on the surface of immune cells and participates in cAMP-PKA, Ca²⁺-calmodulin, PKC and other signaling pathways, producing immunomodulatory effects.

Application of Enkephalins and Proenkephalins

The biological function of ENK plays an important role in the treatment of immune system related diseases and tumor diseases. ENK is involved in the regulation of immune and neuroendocrine systems, has immunomodulatory effects, and is also an important class of cytokines. For diabetic patients with immunodeficiency defects, ENK is expected to serve as a therapeutic to help restore the disordered immune system. ENK has anti-tumor, anti-autoimmune diseases, anti-inflammatory, anti-microbial infections and so on. The functions of ENK analgesic activity, participation in immune regulation, and changes in emotional responses are increasingly attracting attention.

References

1. Chan, D. C. S., Cao, T. H., & Ng, L. L. (2017). Proenkephalin in Heart Failure. Heart failure clinics.
2. Burtscher, J., & Schwarzer, C. (2017). The Opioid System in Temporal Lobe Epilepsy: Functional Role and Therapeutic Potential. Frontiers in molecular neuroscience, 10, 245.