Endomorphin analog analgesics with reduced abuse liability, respiratory depression, motor impairment, tolerance, and glial activation relative to morphine

JE Zadina, MR Nilges, J Morgenweck, X Zhang… - …, 2016 - Elsevier
Opioids acting at the mu opioid receptor (MOR) are the most effective analgesics, however
adverse side effects severely limit their use. Of particular importance, abuse liability results …

Molecular docking of opiates and opioid peptides, a tool for the design of selective agonists and antagonists, and for the investigation of atypical ligand-receptor …

L Gentilucci, A Tolomelli, R De Marco… - Current medicinal …, 2012 - ingentaconnect.com
In the last years, molecular docking emerged as a powerful tool to investigate the
interactions between opioid ligands and their receptors, thus driving the design and …

Strategies to improve bioavailability and in vivo efficacy of the endogenous opioid peptides endomorphin-1 and endomorphin-2

R De Marco, A Janecka - Current Topics in Medicinal …, 2016 - ingentaconnect.com
Morphine and the other alkaloids found in the opium poppy plant still represent the preferred
therapeutic tools to treat severe pain in first aid protocols, as well as chronic pain. The use of …

Design, synthesis, and validation of a β-turn mimetic library targeting protein–protein and peptide–receptor interactions

LR Whitby, Y Ando, V Setola, PK Vogt… - Journal of the …, 2011 - ACS Publications
The design and synthesis of a β-turn mimetic library as a key component of a small-molecule
library targeting the major recognition motifs involved in protein–protein interactions is …

Constraining endomorphin-1 by β, α-hybrid dipeptide/heterocycle scaffolds: identification of a novel κ-opioid receptor selective partial agonist

R De Marco, A Bedini, S Spampinato… - Journal of Medicinal …, 2018 - ACS Publications
Herein we present the expedient synthesis of endomorphin-1 analogues containing
stereoisomeric β2-homo-Freidinger lactam-like scaffolds ([Amo2] EM), and we discuss …

Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potent μ-opioid agonists

X Liu, Y Wang, Y Xing, J Yu, H Ji, M Kai… - Journal of Medicinal …, 2013 - ACS Publications
Recently we reported the synthesis and structure–activity study of endomorphin-1 (EM-1)
analogues containing novel, unnatural α-methylene-β-aminopropanoic acids (Map). In the …

Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration

R Perlikowska, J Piekielna, L Gentilucci… - European journal of …, 2016 - Elsevier
Cyclic pentapeptide Tyr-c [D-Lys-Phe-Phe-Asp] NH 2, based on the structure of
endomorphin-2 (EM-2), which shows high affinity to the μ-opioid receptor (MOR) and a very …

MEL-N16: a series of novel endomorphin analogs with good analgesic activity and a favorable side effect profile

X Liu, L Zhao, Y Wang, J Zhou, D Wang… - ACS chemical …, 2017 - ACS Publications
Opioid peptides are neuromodulators that bind to opioid receptors and reduce pain
sensitivity. Endomorphins are among the most active endogenous opioid peptides, and they …

Controlled Solid Phase Peptide Bond Formation Using N-Carboxyanhydrides and PEG Resins in Water.

R De Marco, A Tolomelli, A Greco… - ACS Sustainable …, 2013 - ACS Publications
The increasing need for large quantities of biologically active peptides for the market
strongly raised the problem of the environmental sustainability of their synthesis. In this …

Novel endomorphin analogues CEMR‐1 and CEMR‐2 produce potent and long‐lasting antinociception with a favourable side effect profile at the spinal level

Y Zhang, S Wang, X Guo, X Liu, X Wang… - British Journal of …, 2024 - Wiley Online Library
Background and Purpose Endomorphins have shown great promise as pharmaceutics for
the treatment of pain. We have previously confirmed that novel endomorphin analogues …