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排序方式: 共有7621条查询结果,搜索用时 25 毫秒
1.
Dr. Elena Petit Dr. Lluís Bosch Prof. Anna M. Costa Ignacio Rodríguez-Izquierdo Dr. Daniel Sepúlveda-Crespo Prof. M. Angeles Muñoz-Fernández Prof. Jaume Vilarrasa 《ChemMedChem》2021,16(14):2217-2222
Amides from indole-3-glyoxylic acid and 4-benzoyl-2-methylpiperazine, which are related to entry inhibitors developed by Bristol-Myers Squibb (BMS), have been synthesized with aliphatic chains located at the C7 position of the indole ring. These spacers contain an azido group suitable for the well-known Cu(I)-catalyzed (3+2)-cycloaddition or an activated triple bond for the nucleophilic addition of thiols under physiological conditions. Reaction with polyols (β-cyclodextrin and hyperbranched polyglycerol) decorated with complementary click partners has afforded polyol-BMS-like conjugates that are not cytotoxic (TZM.bl cells) and retain the activity against R5-HIV-1NLAD8 isolates. Thus, potential vaginal microbicides based on entry inhibitors, which can be called of 4th generation, are reported here for the first time. 相似文献
2.
Gaowa Bai Daisuke Furushima Toshiro Niki Takashi Matsuba Yosuke Maeda Atsushi Takahashi Toshio Hattori Yugo Ashino 《International journal of molecular sciences》2021,22(9)
Numbers of patients with coronavirus disease 2019 (COVID-19) have increased rapidly worldwide. Plasma levels of full-length galectin-9 (FL-Gal9) and osteopontin (FL-OPN) as well as their truncated forms (Tr-Gal9, Ud-OPN, respectively), are representative inflammatory biomarkers. Here, we measured FL-Gal9, FL-OPN, Tr-Gal9, and Ud-OPN in 94 plasma samples obtained from 23 COVID-19-infected patients with mild clinical symptoms (CV), 25 COVID-19 patients associated with pneumonia (CP), and 14 patients with bacterial infection (ID). The four proteins were significantly elevated in the CP group when compared with healthy individuals. ROC analysis between the CV and CP groups showed that C-reactive protein had the highest ability to differentiate, followed by Tr-Gal9 and ferritin. Spearman’s correlation analysis showed that Tr-Gal9 and Ud-OPN but not FL-Gal9 and FL-OPN, had a significant association with laboratory markers for lung function, inflammation, coagulopathy, and kidney function in CP patients. CP patients treated with tocilizumab had reduced levels of FL-Gal9, Tr-Gal9, and Ud-OPN. It was suggested that OPN is cleaved by interleukin-6-dependent proteases. These findings suggest that the cleaved forms of OPN and galectin-9 can be used to monitor the severity of pathological inflammation and the therapeutic effects of tocilizumab in CP patients. 相似文献
3.
Isabel Fernandes Cecília Melo-Alvim Raquel Lopes-Brs Miguel Esperana-Martins Luís Costa 《International journal of molecular sciences》2021,22(2)
Osteosarcoma (OS) is a rare condition with very poor prognosis in a metastatic setting. Basic research has enabled a better understanding of OS pathogenesis and the discovery of new potential therapeutic targets. Phase I and II clinical trials are already ongoing, with some promising results for these patients. This article reviews OS pathogenesis and new potential therapeutic targets. 相似文献
4.
YanXin Dan Takashi Costa Atsushi Nakamura Keiji Komatsu Hidetoshi Saitoh 《Ceramics International》2021,47(9):11862-11869
The morphology and microstructure of splats impact the comprehensive capability of a new coating methodology called chelate flame spraying (CFS). This study addresses the quantitative characterization of the spread morphologies of flame sprayed Er2O3 splats directly deposited under different spray conditions on aluminum alloy substrates with a mirror finish. The influence of the in-flight particle temperature and velocity, carrier gas type, and carrier gas ratio on the solidification mechanism of molten droplets was investigated. Image analysis methods were employed to identify single splats from the morphology observed with field-emission scanning electron microscopy (FE-SEM). In addition, Er2O3 films were synthesized on an Al–Mg alloy (A5052) substrate using N2 or O2 as the carrier gas. When O2 was used as the carrier gas, 109-μm-thick films were deposited on the A5052 substrate. The cross-sectional porosity of the films was 3.8%. In contrast, films with 101-μm thickness were synthesized on the A5052 substrate when N2 was used as the carrier gas. The cross-sectional porosity of these films was 13.8%. The results showed that the carrier gas type (N2) and carrier gas ratio had a significant effect on the flattening behavior of the molten droplets. A spraying method combined with multidimensional modes is proposed to control the morphology of the splats. 相似文献
5.
Takashi Ohnishi Yuki Ogawa Kota Suda Miki Komatsu Satoko Matsumoto Harmon Mitsuru Asukai Masahiko Takahata Norimasa Iwasaki Akio Minami 《International journal of molecular sciences》2021,22(9)
Pyogenic spondylodiscitis can cause severe osteolytic and destructive lesions in the spine. Elderly or immunocompromised individuals are particularly susceptible to infectious diseases; specifically, infections in the spine can impair the ability of the spine to support the trunk, causing patients to be bedridden, which can also severely affect the physical condition of patients. Although treatments for osteoporosis have been well studied, treatments for bone loss secondary to infection remain to be elucidated because they have pathological manifestations that are similar to but distinct from those of osteoporosis. Recently, we encountered a patient with severely osteolytic pyogenic spondylodiscitis who was treated with romosozumab and exhibited enhanced bone formation. Romosozumab stimulated canonical Wnt/β-catenin signaling, causing robust bone formation and the inhibition of bone resorption, which exceeded the bone loss secondary to infection. Bone loss due to infections involves the suppression of osteoblastogenesis by osteoblast apoptosis, which is induced by the nuclear factor-κB and mitogen-activated protein kinase pathways, and osteoclastogenesis with the receptor activator of the nuclear factor-κB ligand-receptor combination and subsequent activation of the nuclear factor of activated T cells cytoplasmic 1 and c-Fos. In this study, we review and discuss the molecular mechanisms of bone loss secondary to infection and analyze the efficacy of the medications for osteoporosis, focusing on romosozumab, teriparatide, denosumab, and bisphosphonates, in treating this pathological condition. 相似文献
6.
Akira Minami Yuuki Kurebayashi Tadanobu Takahashi Tadamune Otsubo Kiyoshi Ikeda Takashi Suzuki 《International journal of molecular sciences》2021,22(6)
Sialidase cleaves sialic acid residues from glycans such as glycoproteins and glycolipids. In the brain, desorption of the sialic acid by sialidase is essential for synaptic plasticity, learning and memory and synaptic transmission. BTP3-Neu5Ac has been developed for sensitive imaging of sialidase enzyme activity in mammalian tissues. Sialidase activity in the rat hippocampus detected with BTP3-Neu5Ac increases rapidly by neuronal depolarization. It is presumed that an increased sialidase activity in conjunction with neural excitation is involved in the formation of the neural circuit for memory. Since sialidase inhibits the exocytosis of the excitatory neurotransmitter glutamate, the increased sialidase activity by neural excitation might play a role in the negative feedback mechanism against the glutamate release. Mammalian tissues other than the brain have also been stained with BTP3-Neu5Ac. On the basis of information on the sialidase activity imaging in the pancreas, it was found that sialidase inhibitor can be used as an anti-diabetic drug that can avoid hypoglycemia, a serious side effect of insulin secretagogues. In this review, we discuss the role of sialidase in the brain as well as in the pancreas and skin, as revealed by using a sialidase activity imaging probe. We also present the detection of influenza virus with BTP3-Neu5Ac and modification of BTP3-Neu5Ac. 相似文献
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9.
Laise Cedraz Pinto Tainá Pinheiro de Oliveira Rayane de Souza Nathane Brito Ferreira Santos Luis Fernandes Pereira Santos Andréa de Assis Santos Teodora Xavier dos Santos Carolaine Teixeira Santos Catarina de Jesus Nunes Isis Barbosa Costa Amanda Catariny de Oliveira Marly Silveira Santos Clícia Maria de Jesus Benevides Mariângela Vieira Lopes 《Journal of Food Processing and Preservation》2021,45(2):e15113
10.
Katarzyna Świrk Paulina Summa Dominik Wierzbicki Monika Motak Patrick Da Costa 《International Journal of Hydrogen Energy》2021,46(34):17776-17783
A series of V-promoted hydrotalcite-derived nickel catalysts (1.0, 2.0, and 4.0 wt%) were tested in CO2 methanation. Ni–I–V2.0 with 2.0 wt% vanadium loading showed the highest catalytic activity, achieving 74.7% of CO2 conversion and 100% of CH4 selectivity at 300 °C. XRD and XANES analyses showed that the smallest Ni0 particles in Ni–I–V2.0 were consistent with the improved textural features observed for this catalyst. Moreover, CO2-TPD revealed the highest sum of weak and medium basic sites in Ni–I–V2.0 that can positively influence catalytic behavior. For the studied catalysts, a clear correlation was demonstrated between the catalytic activity and specific surface area, as well as the basic properties. 相似文献