Transmembrane Allosteric Short Peptides Modulating Human Mu-Opioid Receptor for Analgesic Effects and Covalent Steroid Modifications of Transmembrane Allosteric Peptides for Enhanced Mu-Opioid Receptor Interaction in Chronic Pain Therapies

Abstract: the aspects of the disclosed embodiments introduce a novel class of bioactive compounds, including short peptides and peptidosteroids, designed for the selective modulation of g-protein coupled receptors (gpcrs), with a particular focus on the human mu-opioid receptor (mor). these compounds feature specific amino acid sequences and modifications such as acylation and covalent steroid modifications, including 3beta-hydroxy-5-cholenoic acid or other fatty acid derivatives. these modifications enhance stability, membrane affinity, receptor selectivity, and allosteric modulation potential. the aspects of the disclosed embodiments provide a platform for receptor-targeted therapies, particularly for chronic pain conditions such as neuropathic pain, cancer-related pain, and postoperative pain. by biasing mor signaling toward analgesic pathways and reducing adverse effects, these compounds address the limitations of traditional opioid therapies, offering improved safety, efficacy, and bioavailability. the described peptides and peptidosteroids also exhibit potential for broader gpcr-mediated therapeutic applications, establishing their utility in advancing precision pharmacology.

Inventor(s): Kamil Mieszkowski, Maciej Ciemny

CPC Classification: C07K7/06 (PEPTIDES (peptides in foodstuffs ; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs ; preparations for medicinal purposes ; peptides containing beta-lactam rings ; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, ; ergot alkaloids of the cyclic peptide type ; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids ; macromolecular products derived from proteins ; preparation of glue or gelatine ; single cell proteins, enzymes ; genetic engineering processes for obtaining peptides ; compositions for measuring or testing processes involving enzymes ; investigation or analysis of biological material ))

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