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Dr. Dae-Shik Kim Dr. Atsushi Endo Dr. Francis G. Fang Dr. Kuan-Chun Huang Dr. Xingfeng Bao Dr. Hyeong-wook Choi Dr. Utpal Majumder Dr. Young Y. Shen Steven Mathieu Xiaojie Zhu Kristen Sanders Dr. Thomas Noland Dr. Ming-Hong Hao Dr. Yu Chen Dr. John Y. Wang So Yasui Karen TenDyke Jiayi Wu Christy Ingersoll Kara A. Loiacono Dr. Janna E. Hutz Dr. Nadeem Sarwar 《ChemMedChem》2021,16(11):1741-1744
A strategy for creating potent and pan-genotypic stimulator of interferon genes (STING) agonists is described. Locking a bioactive U-shaped conformation of cyclic dinucleotides by introducing a transannular macrocyclic bridge between the nucleic acid bases leads to a topologically novel macrocycle-bridged STING agonist (MBSA). In addition to substantially enhanced potency, the newly designed MBSAs, exemplified by clinical candidate E7766 , exhibit broad pan-genotypic activity in all major human STING variants. E7766 is shown to have potent antitumor activity with long lasting immune memory response in a mouse liver metastatic tumor model. Two complementary stereoselective synthetic routes to E7766 are also described. 相似文献
3.
Elangeni Ana Gilbert Javier Fernando Guastavino Carolina Guadalupe Gutierrez María Verónica Lancelle Karen Russell-White Marcelo César Murguía 《Journal of surfactants and detergents》2021,24(3):411-419
A novel series of cleavable alkyltrimethylammonium surfactants with different hydrocarbon chain lengths (C8–16) were synthesized. A carbonate break site inserted between the polar head and the hydrocarbon chain makes these compounds hydrolyzable. The reagents used are renewable, (bio)degradable, or reusable. The hydrolysis of these cleavable surfactants will lead to the generation of fatty alcohols and choline, which is an essential biological nutrient. The surface activities in aqueous solution of the synthesized carbonates fulfill the requirement of being good surfactants. In addition, the cleavable compounds containing n-decyl and n-dodecyl chains showed similar or higher antimicrobial activities when compared to a non-cleavable analog. 相似文献
4.
Nina Wurzler Jan D. Schutter Ralph Wagner Matthias Dimper Vasile-Dan Hodoroaba Dirk Lützenkirchen-Hecht Ozlem Ozcan 《工业材料与腐蚀》2021,72(6):983-994
Biofilm formation and microbially influenced corrosion of the iron-reducing microorganism Shewanella putrefaciens were investigated on stainless steel surfaces preconditioned in the absence and presence of flavin molecules by means of XANES (X-ray absorption near-edge structure) analysis and electrochemical methods. The results indicate that biofilm formation was promoted on samples preconditioned in electrolytes containing minute amounts of flavins. On the basis of the XANES results, the corrosion processes are controlled by the iron-rich outer layer of the passive film. Biofilm formation resulted in a cathodic shift of the open circuit potential and a protective effect in terms of pitting corrosion. The samples preconditioned in the absence of flavins have shown delayed pitting and the samples preconditioned in the presence of flavins did not show any pitting in a window of −0.3- to +0.0-V overpotential in the bacterial medium. The results indicate that changes in the passive film chemistry induced by the presence of minute amounts of flavins during a mild anodic polarization can change the susceptibility of stainless steel surfaces to microbially influenced corrosion. 相似文献
5.
Julio E. Trevino Swati Mohan Alexandra E. Salinas Emilia Cueva Karen Lozano 《应用聚合物科学杂志》2021,138(28):50665
This study presents the development and characterization of PVDF-conjugated polymer nanofiber-based systems. Five different conducting polymers (CPs) were synthesized successfully and used to create the nanofiber systems. The CPs used are polyaniline (PANI), polypyrrole (PPY), polyindole (PIN), polyanthranilic acid (PANA), and polycarbazole (PCZ). Nanofiber systems were produced utilizing the Forcespinning® technique. The nanofiber systems were developed by mechanical stretching. No electrical field or post-process poling was used in the nanofiber systems. The morphology, structure, electrochemical and piezoelectric performance was characterized. All of the nanofiber PVDF/CP systems displayed higher piezoelectric performance than the fine fiber PVDF systems. The PVDF/PPY nanofiber system displays the highest piezoelectric performance of 15.56 V. The piezoelectric performance of the PVDF/CP nanofiber systems favors potential for an attractive source of energy where highly flexible membranes could be used in power actuators, sensors and portable, and wireless devices to mention some. 相似文献
6.
Camila C. Lopes Wagner A. Pinheiro Daniel Navarro da Rocha José G. Neves Américo Bortolazzo Correr José R.M. Ferreira Rafael M. Barbosa Jefferson R.F. Soares Jheison L. Santos Marcelo H. Prado da Silva 《Ceramics International》2021,47(6):7653-7665
The repair of bone fractures is a clinical challenge for patients with impaired healing, such as osteoporosis. Currently, different strategies have been developed to design new biomaterials, enhancing their interactions with biological systems and conducting the cellular behavior in the desired direction to help fracture healing. In the present work, hydroxyapatite-graphene oxide (HA-GO) nanocomposites were produced and the morphological and physicochemical influences of the addition of 0.5 wt%, 1.0 wt% and 1.5 wt% of GO to HA were observed. FEG-SEM and TEM analyses of HA-GO nanocomposites showed HA nanoparticles adhered to the surface of the GO sheets, suggesting an effective method to form nanostructured graphene-based biomaterials. As confirmation, physicochemical analyses by Raman, FTIR and TGA demonstrated a strong affinity between HA and GO, according to the increase of concentration from 0.5 wt% to 1.5 wt% GO in the HA-GO nanocomposites. Also, in order to evaluate the HA-GO nanocomposites behavior under biological microenvironment, in vitro bioactivity and indirect cytotoxicity tests were performed. FEG-SEM analyses confirmed the positive results for the bioactivity properties of HA-GO nanocomposite and indirect cytotoxicity demonstrated that even with a decrease in the hDPSCs viability and proliferation, when increasing to 1.5 wt% of GO concentration, high level of cell viability was exhibited by HA-GO nanocomposites. These biological results suggested the 0.5 wt% HA-GO nanocomposite as a potential bioactive bone graft and a promising biomaterial for bone tissue regeneration, when compared to the pure HA. 相似文献
7.
Jonas Stiller Daisy Nestler Husam Ahmad Erik Päßler Guntram Wagner Lothar Kroll 《International Journal of Applied Ceramic Technology》2021,18(2):280-288
The production of ceramic matrix composites (CMC) based on C/C-SiC is still very cost-intensive and therefore only economical for a few applications. The fabrication of the preforms involves many costs that need to be reduced. In this work, the shaping of the CFRP-preforms is realized by thermoset injection molding, which enables large-scale production. The polymeric matrix used is a multi-component matrix consisting of novolak resin, curing agent and lubricant. Six millimeter chopped carbon fiber with a proportion of 50 wt.% were used as a reinforcement. These ingredients are processed by an industrial equipment for compounding and injection molding in order to manufacture a CFRP demonstrator representing a brake disc. Test specimens are cut out of the demonstrator in different directions in order to investigate influences of flow direction and weld lines on microstructural and mechanical properties. Afterward, the CFRP samples were converted to C/C-SiC composites by the liquid silicon infiltration process. The article addresses the flow behavior of the compound during the injection molding and the building of the weld lines in the demonstrator. In addition, results of the directional dependence of the microstructural and mechanical properties within the fabricated disc in the different production steps are presented. 相似文献
8.
Carla C. B. Brasil Cristiano R. de Menezes Eduardo Jacob-Lopes Juliano Smanioto Barin Leila Queiroz Zepka Paulo Cezar Bastianello Campagnol Roger Wagner Alexandre José Cichoski 《International Journal of Food Science & Technology》2020,55(3):1136-1144
This study investigated the effect of the combination of basic electrolysed water (BEW) and slightly acid electrolysed water (SAEW) with ultrasound (US) for cleaning and sanitation of the knives used in slaughtering processes. The knives were sonicated in a US bath using two modes of operation (normal and sweep) in two steps: (i) 5 min with BEW and (ii) 10 min with SAEW at 35 °C. The microbiological counts and the possible changes in the physical structure of the knives were evaluated. The association BEW + SAEW + US, in the sweep mode, provided lower mesophilic, enterobacterial, Staphylococcus aureus and yeast counts when compared to the values recommended by the international legislation. In addition, these conditions removed all organic residues from the knife blades and promoted the highest migration rate of the residues to the US water bath (12.35 mg/L·min), without modifications in the knife blades. Thus, cleaning and sanitation of knives was feasible with the association of BEW + SAEW + US, which could be a useful alternative for the meat industry. 相似文献
9.
Dr. Santina Maiorana Prof. Roberta Ettari Dr. Santo Previti Dr. Giorgio Amendola Dr. Annika Wagner Prof. Sandro Cosconati Prof. Ute A. Hellmich Prof. Tanja Schirmeister Prof. Maria Zappalà 《ChemMedChem》2020,15(16):1552-1561
In this paper, we report the design, synthesis and biological investigation of a series of peptidyl vinyl ketones obtained by modifying the P2 fragment of previously reported highly potent inhibitors of rhodesain, the main cysteine protease of Trypanosoma brucei rhodesiense. Investigation of the structure–activity relationship led us to identify new rhodesain inhibitors endowed with an improved selectivity profile (a selectivity index of up to 22 000 towards the target enzyme), and/or an improved antitrypanosomal activity in the sub-micromolar range. 相似文献
10.
Shana Wagner Megan Waldman Simran Arora Sinan Wang Valerie Scott Dr. Kabirul Islam 《Chembiochem : a European journal of chemical biology》2019,20(9):1133-1138
Histone demethylases play a critical role in mammalian gene expression by removing methyl groups from lysine residues in degree- and site-specific manner. To specifically interrogate members and isoforms of this class of enzymes, we have developed demethylase variants with an expanded active site. The mutant enzymes are capable of performing lysine demethylation with wild-type proficiency, but are sensitive to inhibition by cofactor-competitive molecules embellished with a complementary steric “bump”. The selected inhibitors show more than 20-fold selectivity over the wild-type demethylase, thus overcoming issues typical to pharmacological and genetic approaches. The mutant–inhibitor pairs are shown to act on a physiologically relevant full-length substrate. By engineering a conserved amino acid to achieve member-specific perturbation, this study provides a general approach for studying histone demethylases in diverse cellular processes. 相似文献