144751-75-7Relevant academic research and scientific papers
Towards potential nanoparticle contrast agents: Synthesis of new functionalized PEG bisphosphonates
Kachbi-Khelfallah, Souad,Monteil, Maelle,Cortes-Clerget, Margery,Migianu-Griffoni, Evelyne,Pirat, Jean-Luc,Gager, Olivier,Deschamp, Julia,Lecouvey, Marc
, p. 1366 - 1370 (2016)
The use of nanotechnologies for biomedical applications took a real development during these last years. To allow an effective targeting for biomedical imaging applications, the adsorption of plasmatic proteins on the surface of nanoparticles must be prevented to reduce the hepatic capture and increase the plasmatic time life. In biologic media, metal oxide nanoparticles are not stable and must be coated by biocompatible organic ligands. The use of phosphonate ligands to modify the nanoparticle surface drew a lot of attention in the last years for the design of highly functional hybrid materials. Here, we report a methodology to synthesize bisphosphonates having functionalized PEG side chains with different lengths. The key step is a procedure developed in our laboratory to introduce the bisphosphonate from acyl chloride and tris(trimethylsilyl)phosphite in one step.
Design of nanosystems for the delivery of quorum sensing inhibitors: A preliminary study
Bortolotti, Daria,Cortesi, Rita,Esposito, Elisabetta,Hallan, Supandeep Singh,Marchetti, Paolo,Mariani, Paolo,Rizzo, Roberta,Sguizzato, Maddalena,Trapella, Claudio
, (2021/06/14)
Biofilm production is regulated by the Quorum Sensing system. Nowadays, Quorum Sensing represents an appealing target to design new compounds to increase antibiotics effects and avoid development of antibiotics multiresistance. In this research the use of liposomes to target two novel synthetic biofilm inhibitors is presented, focusing on a preformulation study to select a liposome composition for in vitro test. Five different liposome (LP) formulations, composed of phosphatidyl choline, cholesterol and charged surfactant (2:1:1, molar ratio) have been prepared by direct hydration and extrusion. As charged surfactants dicetyl phosphate didecyldimethylammonium chloride, di isobutyl phenoxy ethyl dimethyl benzyl ammonium chloride and stearylamine (SA) and have been used. Liposome charge, size and morphology were investigated by zeta potential, photon correlation spectroscopy, small angle x-ray spectroscopy and electron microscopy. LP-SA was selected for the loading of biofilm inhibitors and subjected to high performance liquid chromatography for entrapment capacity evaluation. LP-SA loaded inhibitors showed a higher diameter (223.6 nm) as compared to unloaded ones (205.7 nm) and a dose-dependent anti-biofilm effect mainly after 48 h of treatment, while free biofilm inhibitors loose activity. In conclusion, our data supported the use of liposomes as a strategy to enhance biofilm inhibitors effect.
EGFR PROTEOLYSIS TARGETING CHIMERIC MOLECULES AND ASSOCIATED METHODS OF USE
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, (2018/07/29)
The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Creating protein-imprinted self-assembled monolayers with multiple binding sites and biocompatible imprinted cavities
Zhang, Xianfeng,Du, Xuezhong,Huang, Xuan,Lv, Zhongpeng
supporting information, p. 9248 - 9251 (2013/07/25)
Imprinted monolayers have several advantages over bulk imprinted polymers such as excellent mass transfer of molecules into and out of imprinted sites and transduction of binding signals detected in real time. Protein-imprinted self-assembled monolayers (SAMs) were created with multiple binding sites and biocompatible imprinted cavities from functional thiols and novel disulfide compounds containing an oligoethylene glycol (OEG) terminal moiety and two amide groups incorporated in the chain (DHAP) in a biologically benign solution. DHAP played an important role in the formation of multiple binding sites and biocompatible cavities in addition to resisting nonspecific protein binding. The created protein-imprinted SAMs exhibited the excellent ability of specific binding of target proteins determined by multiple binding sites and imprinted cavities. The strategy generates tailor-made monolayer surfaces with specific protein binding and opens the possibility of controlled assembly of intellectual biomaterials and preparation of biosensors.
