A Perfused In Vitro Human iPSC-Derived Blood-Brain Barrier Faithfully Mimics Transferrin Receptor-Mediated Transcytosis of Therapeutic Antibodies.

Delivering biologics to elicit a therapeutic response in the central nervous system (CNS) remains challenging due to the presence of the blood-brain barrier (BBB). Receptor-mediated transcytosis is a strategy to improve brain exposure after systemic drug administration. The availability of a clinically relevant in vitro BBB model is crucial to investigate transcytosis pathways and to predict the penetration of biologics into the CNS.

2-Aminopyridine Analogs Inhibit Both Enzymes of the Glyoxylate Shunt in .

is an opportunistic pathogen responsible for many hospital-acquired infections. can thrive in diverse infection scenarios by rewiring its central metabolism. An example of this is the production of biomass from C nutrient sources such as acetate via the glyoxylate shunt when glucose is not available.

A New Cell-Based AI-2-Mediated Quorum Sensing Interference Assay in Screening of LsrK-Targeted Inhibitors.

Quorum sensing (QS), a bacterial communication strategy, has been recognized as one of the control mechanisms of virulence in bacteria. Thus, targeting QS offers an interesting opportunity to impair bacterial pathogenicity and develop antivirulence agents. Aiming to enhance the discovery of QS inhibitors, we developed a bioreporter Escherichia coli JW5505 pET-Plsrlux and set up a cell-based assay for identifying inhibitors of autoinducer-2 (AI-2)-mediated QS.

Targeting Quorum Sensing: High-Throughput Screening to Identify Novel LsrK Inhibitors.

Since quorum sensing (QS) is linked to the establishment of bacterial infection, its inactivation represents one of the newest strategies to fight bacterial pathogens. LsrK is a kinase playing a key role in the processing of autoinducer-2 (AI-2), a quorum-sensing mediator in gut enteric bacteria. Inhibition of LsrK might thus impair the quorum-sensing cascade and consequently reduce bacterial pathogenicity.

DPD-Inspired Discovery of Novel LsrK Kinase Inhibitors: An Opportunity To Fight Antimicrobial Resistance.

Antibiotic resistance is posing a continuous threat to global public health and represents a huge burden for society as a whole. In the past decade, the interference with bacterial quorum sensing (QS) (i.e.

A Versatile Strategy for the Synthesis of 4,5-Dihydroxy-2,3-Pentanedione (DPD) and Related Compounds as Potential Modulators of Bacterial Quorum Sensing.

Resistance to antibiotics is an increasingly serious threat to global public health and its management translates to significant health care costs. The validation of new Gram-negative antibacterial targets as sources for potential new antibiotics remains a challenge for all the scientists working in this field. The interference with bacterial Quorum Sensing (QS) mechanisms represents a potentially interesting approach to control bacterial growth and pursue the next generation of antimicrobials.

Structure-Based Virtual Screening of LsrK Kinase Inhibitors to Target Quorum Sensing.

In the era of increased antibiotic resistance, targeting enzymes involved in bacterial communication (quorum sensing) represents a new strategy to fight bacterial infections. LsrK is a kinase responsible for the phosphorylation of autoinducer-2, a signaling molecule involved in quorum sensing. Inhibiting LsrK would lead to quorum sensing inactivation and interfere with the pathogenesis.

Nucleobases functionalized quantum dots and gold nanoparticles bioconjugates as a fluorescence resonance energy transfer (FRET) system - Synthesis, characterization and potential applications.

Fluorescence resonance energy transfer (FRET) system based on functionalized CdTe-guanine and AuNPs-cytosine bioconjugates for the model nucleobase - guanine detection was developed. Thioglycolic acid coated cadmium telluride quantum dots (QDs) conjugated with guanine and sodium 3-mercapto-1-propanesulfonate stabilized gold nanoparticles (AuNPs) capped by cytosine were obtained and fully characterized. Successful formation of the materials was confirmed by UV-Vis, fluorescence and FTIR spectroscopies.