Peptides containing β-amino acid patterns: challenges and successes in medicinal chemistry

C Cabrele, TA Martinek, O Reiser… - Journal of Medicinal …, 2014 - ACS Publications
The construction of bioactive peptides using β-amino acid-containing sequence patterns is a
very promising strategy to obtain analogues that exhibit properties of high interest for …

Visible‐Light‐Driven, Copper‐Catalyzed Decarboxylative C(sp3)−H Alkylation of Glycine and Peptides

C Wang, M Guo, R Qi, Q Shang, Q Liu… - Angewandte …, 2018 - Wiley Online Library
Despite a well‐developed and growing body of work in Cu catalysis, the potential of Cu to
serve as a photocatalyst remains underexplored. Reported herein is the first example of …

Endogenous opiates and behavior: 2013

RJ Bodnar - Peptides, 2014 - Elsevier
This paper is the thirty-sixth consecutive installment of the annual review of research
concerning the endogenous opioid system. It summarizes papers published during 2013 …

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 …

Photo-induced preparation of unnatural α-amino acids: synthesis and characterization of novel Leu 5-enkephalin analogues

H Xue, M Guo, C Wang, Y Shen, R Qi, Y Wu… - Organic Chemistry …, 2020 - pubs.rsc.org
We here report the first example of the photo-induced preparation of unnatural α-amino
acids and modification of peptides with unactivated alkyl chlorides (iodides) without the …

Palladium-catalyzed asymmetric allylic amination: enantioselective synthesis of chiral α-methylene substituted β-aminophosphonates

X Wang, X Wang, Z Han, Z Wang, K Ding - Organic Chemistry …, 2017 - pubs.rsc.org
Spiroketal backbone based diphosphine ligands (SKP) were disclosed to be highly efficient
and enantioselective (94→ 99% ee) in the palladium catalyzed asymmetric allylic amination …

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 …

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 …

Intracerebroventricular administration of CYX-6, a potent μ-opioid receptor agonist, a δ-and κ-opioid receptor antagonist and a biased ligand at μ, δ & κ-opioid …

MZ Imam, A Kuo, S Ghassabian, Y Cai, Y Qin… - European Journal of …, 2020 - Elsevier
Mu opioid receptor (MOPr) agonists are thought to produce analgesia via modulation of G-
protein-coupled intracellular signalling pathways whereas the β-arrestin2 pathway is …

Direct inhibition of microglial activation by a μ receptor selective agonist alleviates inflammatory-induced pain hypersensitivity

J Wang, Q Ru, X Yu, C Wang, K Li, N Li, J Zhao… - European Journal of …, 2023 - Elsevier
Opioids are widely used in the treatment of moderate and severe pain. Nociceptive
stimulation has been reported to potentially promote microglial activation and …