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排序方式: 共有312条查询结果,搜索用时 15 毫秒
1.
Antonella Ilenia Alfano Prof. Elisabetta Buommino Prof. Maria Grazia Ferraro Prof. Carlo Irace Prof. Angela Zampella Prof. Heiko Lange Prof. Margherita Brindisi 《ChemMedChem》2021,16(24):3795-3809
The generation of peptidomimetic substructures for medicinal chemistry purposes requires effective and divergent synthetic methods. We present in this work an efficient flow process that allows quick modulation of reagents for Joullié-Ugi multicomponent reaction, using spiroindolenines as core motifs. This sterically hindered imine equivalent could successfully be diversified using various isocyanides and amino acids in generally good space-time yields. A telescoped flow process combining interrupted Fischer reaction for spiroindolenine synthesis and subsequent Joullié-Ugi-type modification resulted in product formation in very good overall yield in less than 2 hours compared to 48 hours required in batch mode. The developed protocol can be seen as a general tool for rapid and facile generation of peptidomimetic compounds. We also showcase preliminary biological assessments for the prepared compounds. 相似文献
2.
Luisa Barbieri Alessandro Bigi Fernanda Andreola Isabella Lancelotti Grazia Ghermandi Maria Teresa Cotes Palomino Carmen Martínez García 《International Journal of Applied Ceramic Technology》2021,18(2):353-368
Within a circular economy approach, this study investigates the environmental impact of lightweight aggregates (LWAs) produced starting from different mixes of different clays with brewery sludge and cattle bone flour ash (CBA), used as poring and fertilizing agents, respectively. The environmental impact was evaluated by means of release tests, insulation capacity, carbon footprint (CFP), and particulate matter emission during pellet firing. Release tests representative of LWAs realistic application showed very high release of phosphate and satisfactory release of potassium. The thermal insulation of the LWAs was tested by thermal imaging camera and resulted highly variable depending on the composition, with the mix containing CBA performing best. This latter composition leads also to the smallest CO2 equivalent emission, due to the calorific power of CBA, allowing lower consumption of fossil fuels during the LWA production. Finally, total particulate emissions during the thermal treatment resulted similar in terms of mass for all mixes, while differences in terms of particle morphology and composition occurred. Samples containing residue resulted with a quite good release behavior, CFP, and insulation properties, but higher emission of particles, particularly when glass is added. 相似文献
3.
Marco Bocchetti Maria Grazia Ferraro Filippo Ricciardiello Alessandro Ottaiano Amalia Luce Alessia Maria Cossu Marianna Scrima Wing-Yan Leung Marianna Abate Paola Stiuso Michele Caraglia Silvia Zappavigna Tung On Yau 《International journal of molecular sciences》2021,22(8)
Colorectal cancer (CRC) is the third most deadly cancer worldwide, and inflammatory bowel disease (IBD) is one of the critical factors in CRC carcinogenesis. IBD is responsible for an unphysiological and sustained chronic inflammation environment favoring the transformation. MicroRNAs (miRNAs) belong to a class of highly conserved short single-stranded segments (18–25 nucleotides) non-coding RNA and have been extensively discussed in both CRC and IBD. However, the role of miRNAs in the development of colitis-associated CRC (CAC) is less clear. The aim of this review is to summarize the major upregulated (miR-18a, miR-19a, miR-21, miR-31, miR-155 and miR-214) and downregulated (miR-124, miR-193a-3p and miR-139-5p) miRNAs in CAC, and their roles in genes’ expression modulation in chronic colonic-inflammation-induced carcinogenesis, including programmed cell-death pathways. These miRNAs dysregulation could be applied for early CAC diagnosis, to predict therapy efficacy and for precision treatment. 相似文献
4.
Elisabetta Coppi Ilaria Dettori Federica Cherchi Irene Bulli Martina Venturini Daniele Lana Maria Grazia Giovannini Felicita Pedata Anna Maria Pugliese 《International journal of molecular sciences》2020,21(24)
Adenosine is a signaling molecule, which, by activating its receptors, acts as an important player after cerebral ischemia. Here, we review data in the literature describing A2BR-mediated effects in models of cerebral ischemia obtained in vivo by the occlusion of the middle cerebral artery (MCAo) or in vitro by oxygen-glucose deprivation (OGD) in hippocampal slices. Adenosine plays an apparently contradictory role in this receptor subtype depending on whether it is activated on neuro-glial cells or peripheral blood vessels and/or inflammatory cells after ischemia. Indeed, A2BRs participate in the early glutamate-mediated excitotoxicity responsible for neuronal and synaptic loss in the CA1 hippocampus. On the contrary, later after ischemia, the same receptors have a protective role in tissue damage and functional impairments, reducing inflammatory cell infiltration and neuroinflammation by central and/or peripheral mechanisms. Of note, demyelination following brain ischemia, or autoimmune neuroinflammatory reactions, are also profoundly affected by A2BRs since they are expressed by oligodendroglia where their activation inhibits cell maturation and expression of myelin-related proteins. In conclusion, data in the literature indicate the A2BRs as putative therapeutic targets for the still unmet treatment of stroke or demyelinating diseases. 相似文献
5.
Bokyung Kim Young Ho Ko Massimiliano Runfola Simona Rapposelli Gabriella Ortore Grazia Chiellini Jin Hae Kim 《International journal of molecular sciences》2021,22(7)
Thyromimetics, whose physicochemical characteristics are analog to thyroid hormones (THs) and their derivatives, are promising candidates as novel therapeutics for neurodegenerative and metabolic pathologies. In particular, sobetirome (GC-1), one of the initial halogen-free thyromimetics, and newly synthesized IS25 and TG68, with optimized ADME-Tox profile, have recently attracted attention owing to their superior therapeutic benefits, selectivity, and enhanced permeability. Here, we further explored the functional capabilities of these thyromimetics to inhibit transthyretin (TTR) amyloidosis. TTR is a homotetrameric transporter protein for THs, yet it is also responsible for severe amyloid fibril formation, which is facilitated by tetramer dissociation into non-native monomers. By combining nuclear magnetic resonance (NMR) spectroscopy, computational simulation, and biochemical assays, we found that GC-1 and newly designed diphenyl-methane-based thyromimetics, namely IS25 and TG68, are TTR stabilizers and efficient suppressors of TTR aggregation. Based on these observations, we propose the novel potential of thyromimetics as a multi-functional therapeutic molecule for TTR-related pathologies, including neurodegenerative diseases. 相似文献
6.
Maria Grazia Basanisi Gianfranco La Bella Gaia Nobili Rosa Coppola Annita Maria Damato Maria Assunta Cafiero Giovanna La Salandra 《International Journal of Food Science & Technology》2020,55(3):1145-1150
The authenticity and traceability of meat products are issues of primary importance to ensure food safety. Unfortunately, food adulteration (e.g. the addition of inexpensive cuts to minced meat products) and mislabelling (e.g. the inclusion of meat from species other than those declared) happens frequently worldwide. The aim of this study was to apply a droplet digital PCR assay for the detection and quantification (copies μL−1) of the beef, pork, horse, sheep, chicken and turkey in meat products. The analysis conducted on commercial meat showed the presence of traces of DNA from other animal species than those declared. We show that the method is highly sensitive, specific and accurate (accuracy = 100%). This method could be adopted by competent food safety authorities to verify compliance with the labelling of meat products and to ensure quality and safety throughout the meat supply chain, from primary production to consumption. 相似文献
7.
8.
Lo Sciuto Grazia Kałużyński Piotr Coco Salvatore 《Journal of Materials Science: Materials in Electronics》2022,33(8):5037-5048
Journal of Materials Science: Materials in Electronics - In this paper, chemiresistor sensor based on conductive polymer (regio-regular poly(3- hexyltiophene) (rr-P3HT) and zinc oxide (ZnO)... 相似文献
9.
Structural and Biochemical Studies of Actin in Complex with Synthetic Macrolide Tail Analogues 下载免费PDF全文
Dr. Jose H. Pereira Dr. Chutima Petchprayoon Dr. Alexander C. Hoepker Dr. Nigel W. Moriarty Dr. Sarah J. Fink Dr. Giuseppe Cecere Prof. Ian Paterson Prof. Paul D. Adams Prof. Gerard Marriott 《ChemMedChem》2014,9(10):2286-2293
The actin filament‐binding and filament‐severing activities of the aplyronine, kabiramide, and reidispongiolide families of marine macrolides are located within the hydrophobic tail region of the molecule. Two synthetic tail analogues of aplyronine C (SF‐01 and GC‐04) are shown to bind to G‐actin with dissociation constants of (285±33) and (132±13) nM , respectively. The crystal structures of actin complexes with GC‐04, SF‐01, and kabiramide C reveal a conserved mode of tail binding within the cleft that forms between subdomains (SD) 1 and 3. Our studies support the view that filament severing is brought about by specific binding of the tail region to the SD1/SD3 cleft on the upper protomer, which displaces loop‐D from the lower protomer on the same half‐filament. With previous studies showing that the GC‐04 analogue can sever actin filaments, it is argued that the shorter complex lifetime of tail analogues with F‐actin would make them more effective at severing filaments compared with plasma gelsolin. Structure‐based analyses are used to suggest more reactive or targetable forms of GC‐04 and SF‐01, which may serve to boost the capacity of the serum actin scavenging system, to generate antibody conjugates against tumor cell antigens, and to decrease sputum viscosity in children with cystic fibrosis. 相似文献
10.
Roberta D’Ambrosio Alessio Aghemo Raffaele De Francesco Maria Grazia Rumi Enrico Galmozzi Stella De Nicola Cristina Cheroni Paul J. Clark Guido Ronchi Pietro Lampertico Massimo Colombo 《International journal of molecular sciences》2014,15(5):7213-7224
The interleukin 28B (IL28B) rs12979860 polymorphism is associated with treatment outcome in hepatitis C virus (HCV) genotype 1 and 4 patients. Its association with the histological features of chronic hepatitis C and disease severity needs further clarifications. To assess the correlation between IL28B genotype, HCV genotype and liver biopsy findings in untreated patients.