Neuropeptides play crucial, mediatory roles in many processes that occur in both CNS and PNS. The commonly accepted
dogma for the release of bioactive peptides involves cleavage of inactive precursor by sequential action of proteinases recognizing dibasic
stretches, followed by truncation of C-terminal Arg/Lys by the carboxypeptidase-like enzyme(s). Dynorphin convertases play an important
role in CNS by regulating dynorphins level and also releasing enkephalins, thus maintaining a balance between these neuropeptides
and their distinct functions (dynorphins are preferentially bound to kappa receptors and enkephalins are directed toward delta receptors).
Knowledge on the cleavage fragments of dynorphins is important for understanding the pharmacological activity of these peptides.
As some new data emerged in the literature, we would like to update recent achievements and progress concerning functions of such convertases,
inhibitors, and their potential role in future pharmacotherapy.
Keywords: Dynorphins, conversion, inhibitors, pharmacology, enzymes, neuropeptides.
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Published on: 17 December, 2012
Page: [1043 - 1051]