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181.
Youri Oh Hoyong Jung Hyejin Kim Jihyun Baek Joonhong Jun Hyunwook Cho Daseul Im Jung-Mi Hah 《International journal of molecular sciences》2021,22(8)
Polo-like kinase 1 (PLK1) plays an important role in cell cycle progression and proliferation in cancer cells. PLK1 also contributes to anticancer drug resistance and is a valuable target in anticancer therapeutics. To identify additional effective PLK1 inhibitors, we performed QSAR studies of two series of known PLK1 inhibitors and proposed a new structure based on a hybridized 3D-QSAR model. Given the hybridized 3D-QSAR models, we designed and synthesized 4-benzyloxy-1-(2-arylaminopyridin-4-yl)-1H-pyrazole-3-carboxamides, and we inspected its inhibitory activities to identify novel PLK1 inhibitors with decent potency and selectivity. 相似文献
182.
Helena Kratochvílov Milo Mrz Barbora J. Kasperov Daniel Hlav
ek Jakub Mahrík Ivana Lakov Anna Cinkajzlov Zdenk Matloch Zdeka Lacinov Jaroslava Trnovsk Peter Ivk Peter Novodvorský Ivan Netuka Martin Haluzík 《International journal of molecular sciences》2021,22(9)
The aim of our study was to analyze mitochondrial and endoplasmic reticulum (ER) gene expression profiles in subcutaneous (SAT) and epicardial (EAT) adipose tissue, skeletal muscle, and myocardium in patients with and without CAD undergoing elective cardiac surgery. Thirty-eight patients, 27 with (CAD group) and 11 without CAD (noCAD group), undergoing coronary artery bypass grafting and/or valvular surgery were included in the study. EAT, SAT, intercostal skeletal muscle, and right atrium tissue and blood samples were collected at the start and end of surgery; mRNA expression of selected mitochondrial and ER stress genes was assessed using qRT-PCR. The presence of CAD was associated with decreased mRNA expression of most of the investigated mitochondrial respiratory chain genes in EAT, while no such changes were seen in SAT or other tissues. In contrast, the expression of ER stress genes did not differ between the CAD and noCAD groups in almost any tissue. Cardiac surgery further augmented mitochondrial dysfunction in EAT. In our study, CAD was associated with decreased expression of mitochondrial, but not endoplasmic reticulum stress genes in EAT. These changes may contribute to the acceleration of coronary atherosclerosis. 相似文献
183.
Gwan Hee Han Ilseon Hwang Hanbyoul Cho Kris Ylaya Jung-A Choi Hyunja Kwon Joon-Yong Chung Stephen M. Hewitt Jae-Hoon Kim 《International journal of molecular sciences》2021,22(11)
Hormone receptor expression patterns often correlate with infiltration of specific lymphocytes in tumors. Specifically, the presence of specific tumor-infiltrating lymphocytes (TILs) with particular hormone receptor expression is reportedly associated with breast cancer, however, this has not been revealed in epithelial ovarian cancer (EOC). Therefore, we investigated the association between hormone receptor expression and TILs in EOC. Here we found that ERα, AR, and GR expression increased in EOC, while PR was significantly reduced and ERβ expression showed a reduced trend compared to normal epithelium. Cluster analysis indicated poor disease-free survival (DFS) in AR+/GR+/PR+ subgroup (triple dominant group); while the Cox proportional-hazards model highlighted the triple dominant group as an independent prognostic factor for DFS. In addition, significant upregulation of FoxP3+ TILs, PD-1, and PD-L1 was observed in the triple dominant group compared to other groups. NanoString analyses further suggested that tumor necrosis factor (TNF) and/or NF-κB signaling pathways were activated with significant upregulation of RELA, MAP3K5, TNFAIP3, BCL2L1, RIPK1, TRAF2, PARP1, and AKT1 in the triple dominant EOC group. The triple dominant subgroup correlates with poor prognosis in EOC. Moreover, the TNF and/or NF-κB signaling pathways may be responsible for hormone-mediated inhibition of the immune microenvironment. 相似文献
184.
Jinhong Kim Junho Jang Sehui Yun Hyeon Deok Kim You Young Byun Yong Tae Park Jung Il Song Chungyeon Cho 《大分子材料与工程》2021,306(9):2100233
In an effort to develop highly functionalized flame retardant materials, hybrid nanocoatings are prepared by alternately depositing a positively charged polyaniline (PANi) and negatively charged montmorillonite (MMT) using the layer-by-layer (LbL) assembly technique. Carbon nanotubes (CNTs) are employed in polymer nanocomposites as effective reinforcement, where nanotubes are stabilized in MMT aqueous solution. The 3D structure and high density of CNTs deposited in the PANi/CNTs-MMT multilayers produce thicker and heavier coatings in comparison to the LbL assemblies without CNTs. Vertical and horizontal flame testing show that the incorporation of CNTs improves fire resistance. Additionally, cone calorimetry reveals that stacking two nanomaterials (MMT and CNTs) in a single coating shows a significant reduction in peak heat release rate (up to 51%), total smoke release (up to 47%), and total heat release (up to 37%) for the polyurethane foam. The enhancement of flame retardancy is attributed to a synergistic effect; MMT serves as a physical barrier that retards the diffusion of heat and gas. The addition of CNTs strengthens the thermal stability and high char yield. These results, coupled with the simplicity with which the LbL deposition is applied, present a viable alternative to halogen-free flame retardant nanocoatings to natural and synthetic fibers. 相似文献
185.
Marine antifouling coating using functional polymers has emerged as an important tool to combat marine fouling. Owing to their natural abundance, polysaccharides represent a more sustainable option than synthetic polymers and carrageenan, a sulfated polysaccharide, is identified as a promising candidate for further research based on its excellent marine antifouling properties. However, existing research has only explored the application of carrageenan-based coatings for 2D objects, using techniques such as spin-coating. Here, a spray-coating method is proposed to apply carrageenan-based coatings to the surfaces of 2- and 3-D objects. The coated surfaces exhibit high stability under various chemical/physical stresses and high resistance to protein adsorption and marine diatom adhesion. 相似文献
186.
Jessica M. Groenevelt Daniel J. Corey Prof. Charlie Fehl 《Chembiochem : a European journal of chemical biology》2021,22(11):1854-1870
All human cells use O-GlcNAc protein modifications (O-linked N-acetylglucosamine) to rapidly adapt to changing nutrient and stress conditions through signaling, epigenetic, and proteostasis mechanisms. A key challenge for biologists in defining precise roles for specific O-GlcNAc sites is synthetic access to homogenous isoforms of O-GlcNAc proteins, a result of the non-genetically templated, transient, and heterogeneous nature of O-GlcNAc modifications. Toward a solution, this review details the state of the art of two strategies for O-GlcNAc protein modification: advances in “bottom-up” O-GlcNAc peptide synthesis and direct “top-down” installation of O-GlcNAc on full proteins. We also describe key applications of synthetic O-GlcNAc peptide and protein tools as therapeutics, biophysical structure–function studies, biomarkers, and as disease mechanistic probes to advance translational O-GlcNAc biology. 相似文献
187.
The effect of thermal shock on the spalling of oxides from the surfaces of several commercial alloys was determined. The average cooling rate was varied from approximately 240°C/sec to less than 1.0°C/sec during cyclic oxidation tests in air. The tests consisted of 100 cycles of 1 hr at the maximimum temperature (1100 or 1200°C). The alloys were HOS-875, TD-Ni, TD-NiCrAl, In-601, In-702, and B-1900 plus Hf. All of these alloys exhibited partial spalling within the oxide rather than total oxide loss down to bare metal. Thermal shock resulted in deformation of the metal, which in turn resulted, in most cases, in change of the oxide failure mode from compressive to tensile. Tensile failures were characterized by cracking of the oxide and little loss, while compressive failures were characterized by explosive loss of platelets of oxide. This behavior was confirmed by examination of mechanically stressed oxide scales. The thermally shocked oxides spalled less than the slow-cooled samples with the exception of TD-NiCrAl. This material failed in a brittle manner rather than by plastic deformation. The HOS-875 and the TD-Ni did not spall during either type of cooling. Thus, the effect of thermal shock on spalling is determined, in large part, by the mechanical properties of the metal. 相似文献
188.
189.
An exact solution inside, outside, and within two arbitrary concentric spherical shells is presented for an impinging monochromatic linearly polarized electromagnetic wave. Specifically, the solution was found for a double-shell spherical acrylic plastic enclosure irradiated with 2450-MHz microwaves. The enclosure is used as an environmentally controlled exposure chamber for experimental animals during microwave irradiation. The analysis shows that an air foamed material, such as styrofoam, would be a better material than either Plexiglas or Teflon, provided it is sufficiently durable. 相似文献
190.
Seung Beom Cho Sridhar Venigalla James H. Adair † 《Journal of the American Ceramic Society》1996,79(1):88-96
Phase-pure, monodispersed, hexagonal plates of single-crystal α-alumina (∼ 2 μm wide and ∼0.5 μm thick) have been prepared via precipitation by treating an aluminum hydrous oxide precursor in 1,4-butanediol at 300°C under autogenous vapor pressure. Present work shows that KOH is the only reagent that precipitates an aluminum hydrous oxide precursor suitable to synthesize α-alumina in 1,4-butanediol solution. In contrast, the use of NaOH or NH4 OH as the precipitating reagent for the precursor material does not yield the alpha phase. The solution pH at which the precursor materials are precipitated is also a critical factor for the formation of α-Al2 O3 . Phase-pure α-alumina powders were also only synthesized from the aluminum hydrous oxide precursors precipitated in the pH range from 10 to 10.5. The results of X-ray diffraction and scanning electron microscopy indicate that longer reaction times promote the phase transformation from the intermediate boehmite phase to α-alumina. The complete transformation from boehmite to α-alumina requires reaction times of about 12 h. 相似文献