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.