Chemoselective reactions for the synthesis of glycoconjugates from unprotected carbohydrates

K Villadsen, MC Martos‐Maldonado, KJ Jensen… - …, 2017 - Wiley Online Library
Glycobiology is the comprehensive biological investigation of carbohydrates. The study of
the role and function of complex carbohydrates often requires the attachment of …

Glycopeptide drugs: A pharmacological dimension between “Small Molecules” and “Biologics”

CR Apostol, M Hay, R Polt - Peptides, 2020 - Elsevier
Peptides are an important class of molecules with diverse biological activities. Many
endogenous peptides, especially neuropeptides and peptide hormones, play critical roles in …

Hypoxia increases expression of selected blood–brain barrier transporters GLUT-1, P-gp, SLC7A5 and TFRC, while maintaining barrier integrity, in brain capillary …

B Ozgür, HCC Helms, E Tornabene… - Fluids and Barriers of the …, 2022 - Springer
Background Brain capillary endothelial cells (BCECs) experience hypoxic conditions during
early brain development. The newly formed capillaries are tight and functional before …

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 …

Multitarget opioid ligands in pain relief: New players in an old game

R Turnaturi, G Aricò, G Ronsisvalle, C Parenti… - European Journal of …, 2016 - Elsevier
Still nowadays pain is one of the most common disabling conditions and yet it remains too
often unsolved. Analgesic opioid drugs, and mainly MOR agonists such as morphine, are …

Structural requirements for CNS active opioid glycopeptides

M Lefever, Y Li, B Anglin, D Muthu… - Journal of Medicinal …, 2015 - ACS Publications
Glycopeptides related to β-endorphin penetrate the blood–brain barrier (BBB) of mice to
produce antinociception. Two series of glycopeptides were assessed for opioid receptor …

Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives

S Deekonda, L Wugalter, D Rankin… - Bioorganic & medicinal …, 2015 - Elsevier
We describe the design and synthesis of novel bivalent ligands based on the conjugation of
4-anilidopiperidine derivatives with enkephalin analogues. The design of non-peptide …

Synthesis and biological evaluation of a library of AGE‐related amino acid triazole crosslinkers

E Icik, A Jolly, P Löffler, N Agelidis… - European Journal of …, 2020 - Wiley Online Library
Three N‐Boc‐protected amino acids, l‐serine, l‐aspartic, and l‐glutamic acid, were either
converted into their methyl azidoalkanoates or various alkynes via Bestmann‐Ohira strategy …

Gram scale production of 1-azido-β-d-glucose via enzyme catalysis for the synthesis of 1, 2, 3-triazole-glucosides

JN Gorantla, S Pengthaisong, S Choknud… - RSC …, 2019 - pubs.rsc.org
The production of analytical amounts of azido sugars is used as a means of verifying
catalytic acid/base mutations of retaining glycosidase, but application of this process to …

Expedient synthesis of N1-substituted triazole peptidomimetics

SB Coffey, G Aspnes, AT Londregan - ACS Combinatorial …, 2015 - ACS Publications
A general procedure for the rapid diversification of peptide scaffolds is described. A one-pot
click reaction between a peptide-alkyne and a series of in situ generated aryl/alkyl azides …