42014-52-8

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Relevant academic research and scientific papers

Phage-Guided Targeting, Discriminative Imaging, and Synergistic Killing of Bacteria by AIE Bioconjugates

New agents with particular specificity toward targeted bacteria and superefficacy in antibacterial activity are urgently needed in facing the crisis of worldwide antibiotic resistance. Herein, a novel strategy by equipping bacteriophage (PAP) with photody

Triazolyl-Based Molecular Gels as Ligands for Autocatalytic ‘Click’ Reactions

The catalytic performance of triazolyl-based molecular gels was investigated in the Huisgen 1,3-dipolar cycloaddition of alkynes and azides. Low-molecular-weight gelators derived from l-valine were synthesized and functionalized with a triazole fragment.

Quaternary diamines as mass spectrometry cleavable crosslinkers for protein interactions

Mapping protein interactions and their dynamics is crucial to defining physiologic states, building effective models for understanding cell function, and to allow more effective targeting of new drugs. Crosslinking studies can estimate the proximity of proteins, determine sites of protein-protein interactions, and have the potential to provide a snapshot of dynamic interactions by covalently locking them in place for analysis. Several major challenges are associated with the use of crosslinkers in mass spectrometry, particularly in complex mixtures. We describe the synthesis and characterization of a MS-cleavable crosslinker containing cyclic amines, which address some of these challenges. The DC4 crosslinker contains two intrinsic positive charges, which allow crosslinked peptides to fragment into their component peptides by collision-induced dissociation (CID) or in-source decay. Initial fragmentation events result in cleavage on either side of the positive charges so crosslinked peptides are identified as pairs of ions separated by defined masses. The structures of the component peptides can then be robustly determined by MS 3 because their fragmentation products rearrange to generate a mobile proton. The DC4 crosslinking reagent is stable to storage, highly reactive, highly soluble (1 M solutions), quite labile to CID, and MS3 results in productive backbone fragmentation.

Charge-Preserving Atom Transfer Radical Polymerization Initiator Rescues the Lost Function of Negatively Charged Protein-Polymer Conjugates

When grown from the surface of proteins, negatively charged polymers cause irreversible inactivation, thereby limiting the breadth of the synthetic space that negatively charged protein-polymer conjugates can be applied to. More broadly speaking, independent of polymer and synthetic approach, almost all protein-polymer conjugates are less active than their precursors. After more than a decade without major advances in understanding why the attachment of some polymers so sharply deactivates enzymes, we focused our attention on a technique to protect enzymes from the growth of a deactivating polymer by restoring the charge at the protein surface during polymer attachment. We synthesized an amino-reactive positively charged atom transfer radical polymerization initiator that inserted a permanent positive charge at the site of bio-macroinitiator attachment. Preserving the surface charge through attachment of the permanent positively charged initiator led to the first observation of activity of enzymes that were coupled to negatively charged homopolymers.

Synthetic strategy to prepare DOTA-based bifunctional chelating agent ready to bind biomolecular probes

Due to the continued interest in new bifunctional chelating agents (BFCA), we focused on the development of a convenient synthesis of 1,4,7,10- tetraazacyclododecane-1,4,7-tris(acetic acid)-10-butyrate mono (N-hydroxysuccinimidyl ester). It consists in the macrocycle DO3A derivatized with an aliphatic linker containing an active ester that requires selective and mild conditions to react with the targeting biomolecule. It is important to underlay the versatility of the obtained BFCA, which can be conjugated both to a biomolecule (protein, Fab fragment) or to a synthetic molecule. In a subsequent step, the developed chelator was successfully conjugated to a peptide sequence.

AGGREGATION INDUCED EMISSION-BACTERIOPHAGE BIOCONJUGATES

Aggregation-induced emission-bacteriophage bioconjugate including a bacteriophage covalently bonded to at least one aggregation-induced emission luminogen via an optional linker, pharmaceutical compositions including the same, and methods of preparation a

AMINO-REACTIVE POSITIVELY CHARGED ATRP INITIATORS THAT MAINTAIN THEIR POSITIVE CHARGE DURING SYNTHESIS OF BIOMACRO-INITIATORS

Provided herein are materials and methods that include utilizing atom transfer radical polymerization (ATRP) initiator molecules that maintain a positive charge during biomacro-initiator synthesis.

Tandem catalysis of an aldol-'click' reaction system within a molecular hydrogel

A heterogeneous supramolecular catalytic system for multicomponent aldol-'click' reactions is reported. The copper(I) metallohydrogel functionalized with a phenyltriazole fragment was able to catalyze the multicomponent reaction between phenylacetylene, p

PHOSPHONATED GLYCOPEPTIDE AND LIPOGLYCOPEPTIDE ANTIBIOTICS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS

The present invention is directed to antimicrobial compounds which have an affinity for binding bones. More particularly, the invention is directed to phosphonated derivatives of glycopeptide or lipoglycopeptide antibiotics. These compounds are useful as antibiotics for the prevention or treatment of bone and joint infections, especially for the prevention and treatment of osteomyelitis.

PROCESS FOR PREPARING NITROOXY ESTERS, NITROOXY THIOESTERS, NITROOXY CARBONATES AND NITROOXY THIOCARBONATES, INTERMEDIATES USEFUL IN SAID PROCESS AND PREPARATION THEREOF

The present invention relates to a process for preparing nitrooxy esters, nitrooxy thioesters, nitrooxy carbonates and nitrooxy thiocarbonates of compounds having at least a hydroxyl or thiol functional group, according to the following reaction scheme, (