Chemical modifications designed to improve peptide stability: incorporation of non-natural amino acids, pseudo-peptide bonds, and cyclization

L Gentilucci, R De Marco… - Current pharmaceutical …, 2010 - ingentaconnect.com
Functions and properties of native peptides vary from highly specific antibiotics or cytotoxic
antitumor drugs, to hormones, neurotransmitters, immunomodulators, etc. Despite their …

Structural chemistry of peptides containing backbone expanded amino acid residues: conformational features of β, γ, and hybrid peptides

PG Vasudev, S Chatterjee, N Shamala… - Chemical …, 2011 - ACS Publications
The remarkable complexity of globular protein structures was first revealed about half a
century ago, when the crystal structure of myoglobin was determined at 2.4 Å. 1 In the …

Opioid receptors and their ligands

A Janecka, J Fichna, T Janecki - Current topics in medicinal …, 2004 - ingentaconnect.com
This review gives a historical perspective, summarizing approximately 25 years of research
on opioids. The “typical” opioid peptides produced in the brain,“atypical” opioids encrypted …

Analgesic opioid ligand discovery based on nonmorphinan scaffolds derived from natural sources

MT Smith, D Kong, A Kuo, MZ Imam… - Journal of Medicinal …, 2022 - ACS Publications
Strong opioid analgesics, including morphine, are the mainstays for treating moderate to
severe acute pain and alleviating chronic cancer pain. However, opioid-related adverse …

[HTML][HTML] Peptidomimetics and their applications for opioid peptide drug discovery

YS Lee - Biomolecules, 2022 - mdpi.com
Despite various advantages, opioid peptides have been limited in their therapeutic uses due
to the main drawbacks in metabolic stability, blood-brain barrier permeability, and …

Endomorphin-1 analogues containing β-proline are μ-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance

G Cardillo, L Gentilucci, AR Qasem… - Journal of medicinal …, 2002 - ACS Publications
In this paper we describe the synthesis and affinity toward the μ-opioid receptor of some
tetrapeptides obtained from endomorphin-1, H-Tyr-Pro-Trp-Phe-NH2 (1), by substituting …

SNew Trends in the Development of Opioid Peptide Analogues as Advanced Remedies for Pain Relief

L Gentilucci - Current topics in medicinal chemistry, 2004 - ingentaconnect.com
The search for new peptides to be used as analgesics in place of morphine has been mainly
directed to develop peptide analogues or peptidomimetics having higher biological stability …

Endomorphins: potential roles and therapeutic indications in the development of opioid peptide analgesic drugs

WX Liu, R Wang - Medicinal research reviews, 2012 - Wiley Online Library
The application of endomorphins as clinical available analgesic drugs has been impeded by
their relatively poor receptor selectivity compared with alkaloid analgesics, rapid …

Enzymatic degradation of endomorphins

A Janecka, R Staniszewska, K Gach, J Fichna - Peptides, 2008 - Elsevier
Centrally acting plant opiates, such as morphine, are the most frequently used analgesics for
the relief of severe pain, even though their undesired side effects are serious limitation to …

[HTML][HTML] Macrocyclic glycopeptides-and derivatized cyclofructan-based chiral stationary phases for the enantioseparation of fluorinated ß-phenylalanine analogs

D Tanács, R Berkecz, S Shahmohammadi… - … of Pharmaceutical and …, 2022 - Elsevier
The enantioseparation of five fluorinated β-phenylalanine analogs together with the
nonfluorinated α-and β-phenylalanines has been investigated utilizing chiral stationary …