Search results for "Phase synthesis"

Synthetic MUC1 Antitumor Vaccine Candidates with Varied Glycosylation Pattern Bearing R/S-configured Pam3 CysSerLys4.

2016

The Toll-like receptor 2 ligand Pam3 CysSer is of particular interest for the construction synthetic vaccines because of its ability to stimulate of the innate immune system. Such vaccines usually comprise Pam3 CysSer with the natural R-configuration at the glycerol 2-position. Pam3 CysSer peptide vaccines with natural configuration have been shown to be more efficient than the corresponding R/S diastereomers. In order to clarify whether the effect of the configuration of Pam3 Cys on the immune response also applies to glycopeptide vaccines, MUC1 glycopeptide-lipopeptide vaccines bearing either R- or R/S-configured Pam3 CysSerLys4 were compared for their immunological effects. In order to f…

Synthesis of Tn/T Antigen MUC1 Glycopeptide BSA Conjugates and Their Evaluation as Vaccines

2011

The tumor-associated mucin MUC1 over-expressed in most epithelial tumor tissues is considered a promising target for immunotherapy. The extracellular part of MUC1 contains a domain of numerous tandem repeats of the amino acid sequence HGVTSAPDTRPAPGSTAPPA, including five potential O-glycosylation sites. In this study, T9 and S15 have been chosen as the positions of glycosylation. The glycopeptides N-terminally equipped with a triethylene glycol spacer were synthesized by microwave-assisted Fmoc solid-phase peptide synthesis. After detachment from the resin and deprotection, the MUC1 glycopeptides were conjugated to bovine serum albumin (BSA). To evaluate the immunological properties, balb/c…

Natural Product Synthesis on Polymeric Supports—Synthesis and Biological Evaluation of an Indolactam Library

1999

Potent activators of protein kinase C in fibroblasts: This property was determined for several indolactam V analogues (1) with a new cell-based assay system. This tumor-promoting indole alkaloid and analogues thereof can be synthesized efficiently on the solid phase. The key steps of the combinatorial approach are a regioselective amination of the indole ring and an enantioselective enzymatic reaction.

Induction of Cell Differentiation in Transformed Keratinocytes by Synthetic (Glyco)peptides from the Homophilic Recognition Domain of E-Cadherin

2002

Litiju saturošu keramiku cietfāžu sintēze un raksturošana

2021

“Litiju saturošu keramiku cietfāžu sintēze un raksturošana”. Seņko M., darba vadītājs vadošais pētnieks Dr. chem. Zariņš A. Zinātniskie konsultanti pētniece, Mg. chem. Avotiņa L. un pētniece, Mg. chem. Trimdale A. Bakalaura darbs, 45 lapas, 31 attēls, 5 tabulas, 54 literatūras avoti, 5 pielikumi. Latviešu valodā. Literatūras apskatā apkopota informācija par procesiem kodoltermiskās sintēzes reaktoros, litiju saturošu savienojumu īpašībām un sintēzes metodēm, raksturotas darbā izmantotās analīžu metodes. Eksperimentālajā daļā ar cietfāžu sintēzes metodi ieguva vairākus litiju saturošus savienojumus, izmantojot dažādus sintēzes parametrus. Fāžu sastāva un termisko īpašību noteikšanai izmantoj…

Synthesis of a polymer-bound galactosylamine and its application as an immobilized chiral auxiliary in stereoselective syntheses of piperidine and am…

2004

A 2,3,4-tri-O-pivaloylated beta-D-galactopyranosyl azide bearing a hydroxy-functionalized spacer unit at the C-6 position of the galactose was synthesized and immobilized on the solid phase by using a polymer-bound chlorosilane. The azide was reduced to the corresponding galactopyranosylamine, which served as a versatile chiral auxiliary in highly diastereoselective Ugi four-component condensation reactions at ambient temperature. Fluoride-induced cleavage from the polymeric support furnished N-glycosylated N-acylated alpha-amino acid amides. The reaction of the immobilized galactosylamine with aldehydes gave rise to the corresponding aldimines, which underwent a domino Mannich-Michael cond…

DNA Block Copolymer Micelles – A Combinatorial Tool for Cancer Nanotechnology

2008

Selective drug targeting of a specific organ or tissue is a challenging task. This holds especially true for chemotherapeutic cancer treatment because most of the available anticancer agents cannot distinguish between cancerous and healthy cells, leading to systemic toxicity and undesirable side effects. One effective approach to address this problem is the application of polymeric nanoparticles equipped with targeting units for tumor-specific delivery. For instance dendrimers, highly branched macromolecules, can be equipped with targeting units as well as with anticancer drugs because of their large number of surface functionalities. Amphiphilic block copolymers, which self-assemble in dil…

Redox-responsive organometallic foldamers from ferrocene amino acid: Solid-phase synthesis, secondary structure and mixed-valence properties

2011

Oligoferrocenes Fmoc-Fca(n)-OMe (n=3-5) are assembled in a stepwise precise manner from Fmoc-protected ferrocene amino acid Fmoc-Fca-OH (H-Fca-OH = 1-amino-1'-ferrocene carboxylic acid; Fmoc = 9-fluorenylmethyloxycarbonyl) via amide bonds on solid supports by sequential Fmoc deprotection, acid activation and coupling steps. The resulting well-defined oligomers form ordered zigzag structures in THF solution with characteristic hydrogen bonding patterns. Electrochemical experiments reveal sequential oxidations of the individual ferrocene units in these peptides giving mixed-valent cations. Optical intervalence electron transfer is detected by intervalence transitions in the near-IR.

Saccharide-induced peptide conformation in glycopeptides of the recognition region of LI-cadherin.

2006

Bioinspired manganese(II) complexes with a clickable ligand for immobilisation on a solid support.

2014

International audience; Clickable ligands like N,N′-bis((pyridin-2-yl)methyl)prop-2-yn-1-amine (L1) and N-((1-methyl-1H-imidazol-2-yl)methyl)-N-(pyridin-2-ylmethyl)prop-2-yn-1-amine (L2) have been used to synthesise a series of manganese(II) complexes for grafting onto appropriate solid supports. These ligands mimic the 2-His-1-carboxylate facial chelation present in the active site of the manganese-dependent dioxygenase (MndD), while the alkyne side function allows grafting of the ligand onto an azido-functionalised support using “click chemistry” methodologies. Such synthetic analogues of the MndD crystallise in the solid state as double halide or pseudohalide-bridged dinuclear manganese(…