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Lee, Y.S. Peptidomimetics and Their Applications for Opioid Peptide Drug. Encyclopedia. Available online: (accessed on 21 April 2024).
Lee YS. Peptidomimetics and Their Applications for Opioid Peptide Drug. Encyclopedia. Available at: Accessed April 21, 2024.
Lee, Yeon Sun. "Peptidomimetics and Their Applications for Opioid Peptide Drug" Encyclopedia, (accessed April 21, 2024).
Lee, Y.S. (2022, November 29). Peptidomimetics and Their Applications for Opioid Peptide Drug. In Encyclopedia.
Lee, Yeon Sun. "Peptidomimetics and Their Applications for Opioid Peptide Drug." Encyclopedia. Web. 29 November, 2022.
Peptidomimetics and Their Applications for Opioid Peptide Drug

Peptidomimetics are synthetically altered peptides with adjusted molecular properties for specific biological or therapeutic applications and have been an important class of drug molecules due to their potential features, high potency, and low toxicity since the term was created first in the late 1970s.

opioid receptors analgesic drugs bioavailability peptidomimetic

1. Opioid Receptors and Natural Opioid Peptides

Opioid receptors which belong to G-protein coupled receptors are known to be involved in pain modulation, numerous physiological functions, and behavioral effects and are characterized in three subtypes, mu- (MOR), delta- (DOR), and kappa-opioid receptor (KOR) with overall 60–65% high structural homology [1]. The extracellular region has much lower homology, and the differences in the region are responsible for the subtype-selectivity of endogenous opioid peptides [2]. There are three main families of the endogenous opioid peptides, END, ENK, and DYN, which are derived from three different precursor proteins, pro-ENK, pro-DYN, and pro-opiomelanocortin, and prefer to bind at the MOR, DOR, and KOR, respectively, with low selectivity but strong analgesic effects in vivo with milder side effects, unlike morphine [1]. Regardless of the receptor selectivity, all of the endogenous opioid peptides share the same N-terminal tetrapeptide sequence (YGGF) that acts as the message part for the receptor, while their C-terminal acts as the address part for selectivity (Table 1).
Table 1. Natural opioid peptides and their selectivities for the opioid receptors.


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