On-resin aggregation and incomplete amide bond formation are major challenges for solid-phase peptide synthesis that are difficult to be monitored in real-time. Incorporation of a pressure-based variable bed flow reactor into an automated solid-phase peptide synthesizer permitted real-time monitoring of resin swelling to determine amino acid coupling efficiency and on-resin aggregation.
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http://dx.doi.org/10.1039/c9cc08421e | DOI Listing |
J Clin Med
January 2025
Institute of Chemistry, Faculty of Materials Science and Engineering, University of Miskolc, 3515 Miskolc, Hungary.
: Subarachnoid hemorrhage is a serious condition caused by ruptured intracranial aneurysms, resulting in severe disability mainly in young adults. Cerebral vasospasm is one of the most common complication of subarachnoid hemorrhage; thus, active prevention is key to improve the prognosis. The glycosylation of proteins is a critical quality attribute which is reportedly altered in patients diagnosed with acute ischemic stroke.
View Article and Find Full Text PDFMolecules
January 2025
School of Health Sciences, Health Campus, Universiti Sains Malaysia, Kubang Kerian 16150, Kelantan, Malaysia.
Malaria, caused by species and transmitted by mosquitoes, continues to pose a significant global health threat. Pipecolisporin, a cyclic hexapeptide isolated from , has emerged as a promising antimalarial candidate due to its potent biological activity and stability. This study explores the synthesis, antimalarial activity, and computational studies of pipecolisporin, aiming to better understand its therapeutic potential.
View Article and Find Full Text PDFBiomedicines
January 2025
Department of Chemistry and Biochemistry, Augusta University, Augusta, GA 30912, USA.
Natural cyclic peptides, a diverse class of bioactive compounds, have been isolated from various natural sources and are renowned for their extensive structural variability and broad spectrum of medicinal properties. Over 40 cyclic peptides or their derivatives are currently approved as medicines, underscoring their significant therapeutic potential. These compounds are employed in diverse roles, including antibiotics, antifungals, antiparasitics, immune modulators, and anti-inflammatory agents.
View Article and Find Full Text PDFChembiochem
January 2025
University of Wisconsin-Madison, Pharmacy, 777 Highland Ave, 53705, Madison, UNITED STATES OF AMERICA.
Peptides and proteins are important functional biomolecules both inside and outside of living organisms. The ability to prepare various types of functionalized peptides and proteins is essential for understanding fundamental biological processes, such as protein folding and post-translational modifications (PTMs), and for developing new therapeutics for many diseases, such as cancers and neurodegenerative diseases. The o-aminoaniline moiety was first proposed for activation to a thioester precursor and used for native chemical ligation to prepare large peptides and proteins.
View Article and Find Full Text PDFEur J Pharmacol
January 2025
Department of Drug and Health Sciences, Pharmacology and Toxicology Section, University of Catania, Italy; Oasi Research Institute-IRCCS, 94018 Troina, Italy. Electronic address:
Background: Adamantane derivatives, such as memantine (Mem) and amantadine (Ada), have distinct mechanisms and therapeutic applications. Ada is primarily utilized as an antiviral and anti-Parkinson drug without significant pro-cognitive effects, Mem is effective in various clinical conditions characterized by cognitive deficits, including Alzheimer's disease. Recent evidence highlights a neuroprotective role for Aβ monomers, suggesting that preventing their aggregation into toxic oligomers could be a promising therapeutic strategy.
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