Search results for "combinatorial"
showing 10 items of 1208 documents
Synthetic multivalent glycopeptide-lipopeptide antitumor vaccines: impact of the cluster effect on the killing of tumor cells.
2014
Multivalent synthetic vaccines were obtained by solid-phase synthesis of tumor-associated MUC1 glycopeptide antigens and their coupling to a Pam3 Cys lipopeptide through click reactions. These vaccines elicited immune responses in mice without the use of any external adjuvant. The vaccine containing four copies of a MUC1 sialyl-TN antigen showed a significant cluster effect. It induced in mice prevailing IgG2a antibodies, which bind to MCF-7 breast tumor cells and initiate the killing of these tumor cells by activation of the complement-dependent cytotoxicity complex.
Correction: One-pot synthesis of a new generation of hybrid bisphosphonate polyoxometalate gold nanoparticles as antibiofilm agents
2019
A reduced polyoxovanadate functionalized with bisphosphonate molecules was synthesized and used to prepare in one step hybrid organic–inorganic polyoxometalate decorated gold nanoparticles. These new composites were shown to strongly inhibit P. aeruginosa and S. epidermidis biofilm growth, with the three components constituting the nanoparticles (Au0 core, vanadium and alendronate) acting synergistically.
Max–min dispersion with capacity and cost for a practical location problem
2022
Diversity and dispersion problems deal with selecting a subset of elements from a given set in such a way that their diversity is maximized. This study considers a practical location problem recently proposed in the context of max–min dispersion models. It is called the generalized dispersion problem, and it models realistic applications by introducing capacity and cost constraints. We propose two effective linear formulations for this problem, and develop a hybrid metaheuristic algorithm based on the variable neighborhood search methodology, to solve real instances. Extensive numerical computational experiments are performed to compare our hybrid metaheuristic with the state-of-art heurist…
Chromogenic detection of nerve agent mimics
2008
The current rise in international concern over criminal terrorist attacks via chemical warfare (CW) agents has resulted in an increasing interest in the detection of these lethal chemicals. Among CW species, nerve agents are extremely dangerous and their high toxicity and ease of production underscore the need to detect these deadly chemicals via quick and reliable procedures. A number of detection systems have been developed, most of them based on enzymatic and physical methodologies. However, these usually show limitations such as low selectivity, lack of portability and a certain complexity in their use. An alternative to these classical methods that has been gaining interest in recent y…
Energy efficient resource allocation in heterogeneous software defined network: A reverse combinatorial auction approach
2015
In this paper, resource allocation for energy effi- ciency in heterogeneous Software Defined Network (SDN) with multiple network service providers (NSPs) is studied. The considered problem is modeled as a reverse combinatorial auction game, which takes different quality of service (QoS) requirements into account. The heterogeneous network selection associated with power allocation problem is optimized by maximizing the energy efficiency of data transmission. By exploiting the properties of fractional programming, the resulting non-convex Winner Determination Problem (WDP) is transformed into an equivalent subtractive convex optimization problem. The proposed reverse combinatorial auction ga…
[60]Fullerene l -Amino Acids and Peptides: Synthesis under Phase-Transfer Catalysis Using a Phosphine–Borane Linker. Electrochemical Behavior
2017
International audience; A new method to link amino acid and peptide derivatives to [60]fullerene is described. It uses hydrophosphination with a secondary phosphine borane. First, the stereoselective synthesis of secondary phosphine borane amino acid derivatives was achieved by alkylation of phenylphosphine borane with gamma-iodo-alpha-amino ester reagents under phase transfer catalysis (PTC). Second, a sec-phosphine borane amino ester was saponified and coupled with alpha,gamma-diamino esters to afford the corresponding dipeptide derivatives in good yields. Finally, the hydrophosphination reaction of [60]fullerene by the sec-phosphine borane compounds was performed under PTC to obtain C-60…
Trans -Cyclooctene-Functionalized PeptoBrushes with Improved Reaction Kinetics of the Tetrazine Ligation for Pretargeted Nuclear Imaging
2020
Tumor targeting using agents with slow pharmacokinetics represents a major challenge in nuclear imaging and targeted radionuclide therapy as they most often result in low imaging contrast and high radiation dose to healthy tissue. To address this challenge, we developed a polymer-based targeting agent that can be used for pretargeted imaging and thus separates tumor accumulation from the imaging step in time. The developed targeting agent is based on polypeptide-graft-polypeptoid polymers (PeptoBrushes) functionalized with trans-cyclooctene (TCO). The complementary In-111-labeled imaging agent is a 1,2,4,5-tetrazine derivative, which can react with aforementioned TCO-modified PeptoBrushes i…
High-affinity and selective detection of pyrophosphate in water by a resorcinarene salt receptor
2017
N-Alkyl ammonium resorcinarenes selectively bind pyrophosphate in pure water with an exceptionally high binding constant of up to 1.60 × 107 M–1, three orders of magnitude higher than ATP.
Synthesis and biological evaluation of novel peptidomimetics as rhodesain inhibitors
2016
Novel rhodesain inhibitors were developed by combining an enantiomerically pure 3-bromoisoxazoline warhead with a 1,4-benzodiazepine scaffold as specific recognition moiety. All compounds were proven to inhibit rhodesain with Ki values in the low-micromolar range. Their activity towards rhodesain was found to be coupled to an in vitro antitrypanosomal activity, with IC50 values ranging from the mid-micromolar to a low-micromolar value for the most active rhodesain inhibitor (R,S,S)-3. All compounds showed a good selectivity against the target enzyme since all of them were proven to be poor inhibitors of human cathepsin L. Novel rhodesain inhibitors were developed by combining an enantiomeri…
Structural Motifs of Alkali Metal Superbases in Non‐coordinating Solvents
2020
Abstract Lochmann–Schlosser superbases (LSB) are a standard reagent in synthetic chemistry to achieve an exchange of a proton on an organic framework with an alkali metal cation, which in turn can be replaced by a wide range of electrophilic groups. In standard examples, the deprotonating reagent consists of an equimolar mixture of n‐butyllithium and potassium t‐butoxide. However, the nature of the reactive species could not be pinned down either for this composition or for similar mixtures with comparable high reactivity. Despite the poor solubility and the fierce reactivity, some insights into this mixture were achieved by some indirect results, comparison with chemically related systems,…