Search results for " Conjugate"

Free and conjugated polyamine content in Citrus sinensis Osbeck, cultivar Brasiliano N.L.92, a Navel orange, at different maturation stages

2004

Biogenic amines, synthesized during physiological metabolic processes of all living organisms, are present in food. At low concentrations, polyamines are essential for cell renewal and growth, but they can be detrimental when consumed in high amount through the diet as they could support abnormal cell growth pathologies. The daily human diet contains more putrescine than spermidine or spermine, mostly derived from fruits. In general, orange fruits contain high levels of put, a fact that could limit their utilization in the daily diet besides the benefits contributed by their strong antioxidant properties. There is therefore an increasing interest in finding plant foods with low polyamine co…

Chemical Strategies for the Synthesis of Protein–Polymer Conjugates

2012

Protein-polymer conjugates have achieved tremendous attention in the last few years. The synergistic combination of properties has led to certain advantages in bio-applications. Over the past few years, numerous chemical strategies have been developed to conjugate different synthetic polymers onto proteins, most of which can be summarized within the scope of click-chemistry. Here we highlight conjugation strategies based on available functional groups present on the synthetic polymer and existing groups of proteins from the natural pool. In particular, the chapter organizes the various possible reactions by classes of functional groups present on protein surfaces, deriving from selected ami…

(p-Sulfomethyl)phenylalanine as a mimic of O-sulfatyl-tyrosine in synthetic partial sequences of P-Selectin glycoprotein ligand 1 (PSGL-1)

2007

Abstract Fmoc- l -( p -sulfomethyl)phenylalanine, a bioisosteric mimic of acid-sensitive O -sulfatyl tyrosine, was synthesized from l -tyrosine according to a novel route. Partial sequences of the recognition site of P-Selectin glycoprotein ligand 1 (PSGL-1), which contain (sulfomethyl)phenylalanine were synthesized on solid-phase. By fragment condensation, a sialyl Lewis x peptide conjugate containing a (sulfomethyl)phenylalanine mimic of O -sulfatyl tyrosine was prepared without destruction of the acid-sensitive fucoside bond within the saccharide side chain. Compounds of this type are of interest as sufficiently acid-stable potential inhibitors of P-Selectin in inflammatory processes.

Chemical conjugation of dexamethasone to a polyaspartamide and in vitro evaluation studies

2004

Two macromolecular conjugates of dexamethasone containing different drug amounts were synthesized using PHEA as the polymeric carrier and a succinic group as spacer. The content of linked drug was equal to 25.3% w/w (conjugate A) and 12.7% w/w (conjugate B). Both polymeric conjugates, unlike the free drug, were water-soluble and the amount of unlinked drug was evaluated to be approximately about 0.01% w/w. Both conjugates were relatively stable in vitro at pH 7.4 whereas in the presence of esterase only the conjugate B was able to release drug under the used experimental conditions. This dissimilar behavior has been attributed to the distinct macromolecular conformations assumed in aqueous …

Isomerization of 9c11t/10t12c CLA in Triacylglycerols

2010

Published version of an article in the journal: Lipids . The original publication is available at Spingerlink. http://dx.doi.org/10.1007/s11745-010-3452-x Isomers of conjugated linoleic acid from 7t9c through 12t14t can be induced by thermal treatment of triacylglycerol samples of 9c11t or 10t12c fatty acids in glass tubes. The formation of conjugated linoleic acids (CLAs) has been observed during thermal induction of the above-mentioned triacylglycerols at 250, 280 and 320A degrees C. The concentrations of isomers formed in the mixture varied depending on the temperature and duration of the heating experiments. The objective of this study was to find a suitable thermal induction temperatur…

New amphiphilic conjugates of mono- and bis(carboxy)-PEG(2,000) polymers with lipoamino acids as surface modifiers of colloidal drug carriers

2010

Structure and properties of pharmacologically active polymers

1975

Although the concept of using pharmacologically active macromolecular compounds as drugs is still regarded with much skepticism for both theoretical and practical reasons, interest in this field has grown in recent years because of the opportunity to take advantage of the specific properties of polymeric materials. For low molecular weight drugs, changes in structure often lead to a loss of specific activity. On the other hand, the properties of macromolecular drugs depend on the structure of the polymer used and this can be varied over a wide range by the incorporation of comonomer units, by the application of polymer-analogous reactions, or by related structural changes. A new model is pr…

First Chemosensor for Selective Detection and Quantification of L-4-Hydroxyproline in Collagen and Other Bio Samples.

2017

Amino pyridine-based rhodamine conjugate (APR) has been developed as a first chemosensor for selective detection and quantification of L-4-Hydroxyproline (Hyp). The “turn-on” fluorescence property of the chemosensor makes it unique for easy estimation of Hyp in collagen and biological samples. peerReviewed

Antibody-drug conjugates for lymphoma patients: preclinical and clinical evidences

2022

Antibody-drug conjugates (ADCs) are a recent, revolutionary approach for malignancies treatment, designed to provide superior efficacy and specific targeting of tumor cells, compared to systemic cytotoxic chemotherapy. Their structure combines highly potent anti-cancer drugs (payloads or warheads) and monoclonal antibodies (Abs), specific for a tumor-associated antigen, via a chemical linker. Because the sensitive targeting capabilities of monoclonal Abs allow the direct delivery of cytotoxic payloads to tumor cells, these agents leave healthy cells unharmed, reducing toxicity. Different ADCs have been approved by the US Food and Drug Administration (FDA) and the European Medicines Agency (…

Synthesis of a MUC1-glycopeptide-BSA conjugate vaccine bearing the 3'-deoxy-3'-fluoro-Thomsen-Friedenreich antigen.

2011

A novel MUC1-glycopeptide–BSA conjugate vaccine with a specifically fluorinated Thomsen–Friedenreich antigen side chain at Thr6 was prepared. Preliminary immunological experiments reveal specific binding of the tumor-associated glycopeptide antigen analog by anti-MUC1-mouse antibodies.