排序方式: 共有39条查询结果,搜索用时 15 毫秒
1.
2.
Synthesis and Biochemical Evaluation of Warhead-Decorated Psoralens as (Immuno)Proteasome Inhibitors
Eva Shannon Schiffrer Matic Proj Martina Gobec Luka Rejc Andrej terman Janez Mravljak Stanislav Gobec Izidor Sosi
《Molecules (Basel, Switzerland)》2021,26(2)
The immunoproteasome is a multicatalytic protease that is predominantly expressed in cells of hematopoietic origin. Its elevated expression has been associated with autoimmune diseases, various types of cancer, and inflammatory diseases. Selective inhibition of its catalytic activities is therefore a viable approach for the treatment of these diseases. However, the development of immunoproteasome-selective inhibitors with non-peptidic scaffolds remains a challenging task. We previously reported 7H-furo[3,2-g]chromen-7-one (psoralen)-based compounds with an oxathiazolone warhead as selective inhibitors of the chymotrypsin-like (β5i) subunit of immunoproteasome. Here, we describe the influence of the electrophilic warhead variations at position 3 of the psoralen core on the inhibitory potencies. Despite mapping the chemical space with different warheads, all compounds showed decreased inhibition of the β5i subunit of immunoproteasome in comparison to the parent oxathiazolone-based compound. Although suboptimal, these results provide crucial information about structure–activity relationships that will serve as guidance for the further design of (immuno)proteasome inhibitors. 相似文献
3.
Ruocco G Matic A Scopigno T Yannopoulos SN 《Physical review letters》2007,98(7):079601; author reply 079602
4.
The acoustic branch of two network glasses, (Li2O)xB2O3 ( x = 0.25 and 0.5), is followed over a large momentum transfer range 1-12 nm(-1), using inelastic x-ray scattering. We observe the transition from propagating modes to a region of strong scattering as the Ioffe-Regel limit is reached. A region of Rayleigh scattering of the acoustic modes precedes the strong scattering regime at larger Q, causing a rapid decrease of the mean-free path of the modes. 相似文献
5.
A failure criterion is presented which relates the strain energy density of the material to both yielding and fracture. Cumulative material damage throughout a structural component may be monitored and the relative influence of yielding and stable crack growth assessed. The criterion is demonstrated, using finite element analysis, for center cracked panel specimens differing by material toughness values. From crack growth increment predictions using the uniaxial stress-strain behavior of the material, the criterion predicts the critical value of the strain energy density factor Sc governing crack instability. 相似文献
6.
A statistical analysis of findings in assessments by an accreditation body, external audits and internal audits in an accredited testing laboratory for gamma-ray spectrometry is presented. The frequencies of observations reported in different areas were examined and analysed. The differences are interpreted in terms of the varying importance associated with the different areas as perceived by auditors and assessors. 相似文献
7.
A. Stern S.R. Kreitzman A. Resnik D. Shaltiel V. Zevin 《Solid State Communications》1981,40(8):837-841
Thermal desorption of hydrogen from the bulk of the system ZrV2Hx, 0.3 ? x ? 4.27, shows spectra which develop from a single peak, for x < 1, to a spectrum that consists of 3 peaks and a shoulder for x ? 4.27. A model is proposed to explain the origin of these peaks and relates them to a consecutive desorption of the hydrogens from the different interstitial sites, in agreement with neutron diffraction data on the sites' occupancy. However, neutron diffraction indicates that up to x ≈ 2.5 the hydrogens occupy the tetrahedral sites formed by 2 Zr and 2 V, nevertheless our results show that there is a large difference in the bonding energy of these sites for hydrogens with x < 1 and hydrogens with 1 < x < 2.5. 相似文献
8.
Matic Lozinšek Evgeny Goreshnik Anton Meden Gašper Tav?ar 《Journal of solid state chemistry》2009,182(10):2897-2903
In the system BaF2/BF3/PF5/anhydrous hydrogen fluoride (aHF) a compound Ba(BF4)(PF6) was isolated and characterized by Raman spectroscopy and X-ray diffraction on the single crystal. Ba(BF4)(PF6) crystallizes in a hexagonal space group with a=10.2251(4) Å, c=6.1535(4) Å, V=557.17(5) Å3 at 200 K, and Z=3. Both crystallographically independent Ba atoms possess coordination polyhedra in the shape of tri-capped trigonal prisms, which include F atoms from BF4− and PF6− anions. In the analogous system with AsF5 instead of PF5 the compound Ba(BF4)(AsF6) was isolated and characterized. It crystallizes in an orthorhombic Pnma space group with a=10.415(2) Å, b=6.325(3) Å, c=11.8297(17) Å, V=779.3(4) Å3 at 200 K, and Z=4. The coordination around Ba atom is in the shape of slightly distorted tri-capped trigonal prism which includes five F atoms from AsF6− and four F atoms from BF4− anions. When the system BaF2/BF3/AsF5/aHF is made basic with an extra addition of BaF2, the compound Ba2(BF4)2(AsF6)(H3F4) was obtained. It crystallizes in a hexagonal P63/mmc space group with a=6.8709(9) Å, c=17.327(8) Å, V=708.4(4) Å3 at 200 K, and Z=2. The barium environment in the shape of tetra-capped distorted trigonal prism involves 10 F atoms from four BF4−, three AsF6− and three H3F4− anions. All F atoms, except the central atom in H3F4 moiety, act as μ2-bridges yielding a complex 3-D structural network. 相似文献
9.
Bacterial infections of medical devices present severe problems connected with long-term antibiotic treatment, implant failure, and high hospital costs. Therefore, there are enormous demands for innovative techniques which would improve the surface properties of implantable materials. Plasma technologies present one of the compelling ways to improve metal’s antibacterial activity; plasma treatment can significantly alter metal surfaces’ physicochemical properties, such as surface chemistry, roughness, wettability, surface charge, and crystallinity, which all play an important role in the biological response of medical materials. Herein, the most common plasma treatment techniques like plasma spraying, plasma immersion ion implantation, plasma vapor deposition, and plasma electrolytic oxidation as well as novel approaches based on gaseous plasma treatment of surfaces are gathered and presented. The latest results of different surface modification approaches and their influence on metals’ antibacterial surface properties are presented and critically discussed. The mechanisms involved in bactericidal effects of plasma-treated surfaces are discussed and novel results of surface modification of metal materials by highly reactive oxygen plasma are presented. 相似文献
10.
Concentration effects on irreversible colloid cluster aggregation and gelation of silica dispersions
Schantz Zackrisson A Martinelli A Matic A Bergenholtz J 《Journal of colloid and interface science》2006,301(1):137-144
Effects of particle concentration on the irreversible aggregation of colloidal silica are studied using in situ destabilization via the ionic strength increase derived from the enzymatic hydrolysis of urea by urease. Aggregation is monitored by time-resolved optical density and dynamic light scattering measurements. It terminates at a gel boundary, signaled by a prominent increase of the optical density and incipient non-ergodicity. Raman scattering is used to demonstrate that the enzymatic reaction continues, well beyond gelation for the compositions studied here, until the urea is consumed. Calibration of the ionic conductivity permits for constructing stability diagrams in terms of particle and salt concentration. As with reversible gelation, the process exhibits a collective character in that lower ionic strengths are required for gelation of concentrated dispersions and vice versa. However, light scattering demonstrates that the gel boundary is preceded here by a line marking the transition from reversible to irreversible cluster formation, with the two transition boundaries tracking each other. Comparisons are made with dispersions destabilized by direct addition of salt solutions, which gel under very different conditions. 相似文献