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 …
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 …
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 …
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
Strong opioid analgesics, including morphine, are the mainstays for treating moderate to
severe acute pain and alleviating chronic cancer pain. However, opioid-related adverse …
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 …
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 …
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 …
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 …
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 …
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 …
nonfluorinated α-and β-phenylalanines has been investigated utilizing chiral stationary …