Synthesis of a tricyclic hexapeptide –via two consecutive ruthenium-catalyzed macrocyclization steps– with a constrained topology to mimic vancomycin's binding properties toward D-Ala-D-Ala dipeptide

A ring-closing metathesis (RCM) - peptide coupling - ruthenium-catalyzed azide alkyne cycloaddition (RuAAC) strategy was developed to synthesize a tricyclic hexapeptide in which the side chain to side chain connectivity pattern resulted in a mimic with a topology that effectively mimics the bioactivity of vancomycin as a potent binder of the bacterial cell wall D-Ala-D-Ala dipeptide sequence and more importantly being an effective inhibitor of bacterial growth

Формування органів управління кінематографа в Україні (1919)

У статті розглядається процес створення та діяльність органів управління кінематографа в перші роки функціонування радянської влади в Україні.В статье рассматривается процесс создания и деятельность органов управления кинематографа в первые годы функционирования советской власти в Украине.The process of creating and functioning of the cinematography authorities in the early years of the Soviet Union in Ukraine is examined in the article

Synthesis of 1,5-triazole bridged vancomycin CDE-ring bicyclic mimics using RuAAC macrocyclization

Herein we report the Ru(<sub>II</sub>)-catalyzed double-macrocyclization of a hexapeptide to obtain a mimic of the bicyclic CDE-ring of vancomycin, followed by measurement of its binding affinity for small peptide ligands using ITC

A sustainable approach to inward investment?

Also known as Insights publication seriesAvailable from British Library Document Supply Centre-DSC:4024.086045(3) / BLDSC - British Library Document Supply CentreSIGLEGBUnited Kingdo

Synthesis of cyclic peptides via transition metal catalyzed C-C bond formation

No abstract available

Change in the financial sector and trends in housing finance markets

SIGLEAvailable from British Library Document Supply Centre-DSC:GPE/0163 / BLDSC - British Library Document Supply CentreGBUnited Kingdo

Mirror image supramolecular helical tapes formed by the enantiomeric-depsipeptide derivatives of the amyloidogenic peptide amylin(20-29)

Factors that determine the chirality of supramolecular helical tapes formed by a backbone-modified amylin(20-29) depsipeptide and inverso-depsipeptide, were studied by Fourier transform infrared spectroscopy, circular dichroism and transmission electron microscopy. Although P-sheet propensity was absent in both peptides, it was found that the L-depsipeptide formed left-handed and the enantiomeric D-depsipeptide right-handed helical tapes. Moreover, the backbone-modified depsipeptides, showed a certain degree of cross-recognition between both enantiomers, which might have implications in designing amyloid formation inhibitors. (c) 2007 Elsevier Ltd. All rights reserved

Inhibition of Octreotide Acylation Inside PLGA Microspheres by Derivatization of the Amines of the Peptide with a Self-Immolative Protecting Group

Acylation of biopharmaceuticals such as peptides has been identified as a major obstacle for the successful development of PLGA controlled release formulations. The purpose of this study was to develop a method to inhibit peptide acylation in poly(d,l-lactide-co-glycolide) (PLGA) formulations by reversibly and temporarily blocking the amine groups of a model peptide (octreotide) with a self-immolative protecting group (SIP), O-4-nitrophenyl-O'-4-acetoxybenzyl carbonate. The octreotide with two self-immolative protecting groups (OctdiSIP) on the N-terminus and lysine side chain was synthesized by reaction of the peptide with O-4-nitrophenyl-O'-4-acetoxybenzyl carbonate, purified by preparative RP-HPLC and characterized by mass spectrometry. Degradation studies of OctdiSIP in aqueous solutions of different pH values showed that protected octreotide was stable at low pH (pH 5) whereas the protecting group was eliminated at physiological pH, especially in the presence of an esterase, to generate native octreotide. OctdiSIP encapsulated in PLGA microspheres, prepared using a double emulsion solvent evaporation method, showed substantial inhibition of acylation as compared to the unprotected octreotide: 52.5% of unprotected octreotide was acylated after 50 days incubation of microspheres in PBS pH 7.4 at 37 °C, whereas OctdiSIP showed only 5.0% acylation in the same time frame. In conclusion, the incorporation of self-immolative protection groups provides a viable approach for inhibition of acylation of peptides in PLGA delivery systems