Design, Synthesis, and Biological Evaluation of the Quorum-Sensing Inhibitors of PAO1.

Due to the resistance of Gram-negative bacteria PAO1 to most clinically relevant antimicrobials, the use of traditional antibiotic treatments in hospitals is challenging. The formation of biofilms, which is regulated by the quorum-sensing (QS) system of (PA), is an important cause of drug resistance. There are three main QS systems in : the system, the system, and the system.

Discovery of Novel STING Inhibitors Based on the Structure of the Mouse STING Agonist DMXAA.

The stimulator-of-interferon-gene (STING) protein is involved in innate immunity. The drug DMXAA (5,6-dimethylxanthenone-4-acetic acid) proved to be a potent murine-STING (mSTING) agonist but had little effect on human-STING (hSTING). In this paper, we draw upon the comparison of different crystal structures and protein-ligand interaction relationships analysis to venture the hypothesis that the drug design of DMXAA variants has the potential to convert STING agonists to inhibitors.

Eukaryotic initiation factor 6 repression mitigates atherosclerosis progression by inhibiting macrophages expressing Fasn.

Atherosclerosis, a chronic inflammatory disease that often leads to myocardial infarction and stroke, is mainly caused by lipid accumulation. Eukaryotic initiation factor 6 (Eif6) is a rate-limiting factor in protein translation of transcription factors necessary for lipogenesis. To determine whether Eif6 affects atherosclerosis, Eif6+/- mice were crossed into Apoe-/- background.

Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonists.

STING (Stimulator of Interferon Genes) has become a focal point in immunology research and a target in drug discovery. The discovery of a potent human-STING agonist is expected to revolutionize current anti-virus or cancer immunotherapy. Inspired by the structure and function of murine STING-specific agonists (DMXAA and CMA), we rationally designed and synthesized four series of novel compounds for the enhancement of human sensitivity.

Bv8-Like Toxin from the Frog Venom of Promotes Wound Healing via the Interleukin-1 Signaling Pathway.

Prokineticins are highly conserved small peptides family expressed in all vertebrates, which contain a wide spectrum of functions. In this study, a prokineticin homolog (Bv8-AJ) isolated from the venom of frog was fully characterized. Bv8-AJ accelerated full-thickness wounds healing of mice model by promoting the initiation and the termination of inflammatory phase.

Dicke-type phase transition in a spin-orbit-coupled Bose-Einstein condensate.

Spin-orbit-coupled Bose-Einstein condensates (BECs) provide a powerful tool to investigate interesting gauge field-related phenomena. Here we study the ground state properties of such a system and show that it can be mapped to the well-known Dicke model in quantum optics, which describes the interactions between an ensemble of atoms and an optical field. A central prediction of the Dicke model is a quantum phase transition between a superradiant phase and a normal phase.

Efficient fluorescent chemosensors for HSO4(-) based on a strategy of anion-induced rotation-displaced H-aggregates.

A novel fluorometric sensing strategy based on the anion-induced rotation-displaced H-aggregates of styrylindolium dyes was employed to enhance the selectivity of fluorescent chemosensors for HSO4(-) detection. The marvelous anion-induced H-aggregate strategy opens new routes to simple synthesis of receptors for tetrahedral anionic species.