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61.
Rationally Designed Semisynthetic Natural Product Analogues for Stabilization of 14‐3‐3 Protein–Protein Interactions 下载免费PDF全文
Sebastian A. Andrei Pim de Vink Eline Sijbesma Ling Han Prof. Luc Brunsveld Prof. Nobuo Kato Prof. Christian Ottmann Dr. Yusuke Higuchi 《Angewandte Chemie (International ed. in English)》2018,57(41):13470-13474
The natural product family of fusicoccanes are stabilizers of 14‐3‐3 mediated protein–protein interactions (PPIs), some of which possess antitumor activity. In this study, the first use of molecular dynamics (MD) to rationally design PPI stabilizers with increased potency is presented. Synthesis of a focused library, with subsequent characterization by fluorescence polarization, mutational studies, and X‐ray crystallography confirmed the power of the MD‐based design approach, revealing the potential for an additional hydrogen bond with the 14‐3‐3 protein to lead to significantly increased potency. Additionally, these compounds exert their action in a cellular environment with increased potency. The newly found polar interaction could provide an anchoring point for new small‐molecule PPI stabilizers. These results facilitate the development of fusicoccanes towards drugs or tool compounds, as well as allowing the study of the fundamental principles behind PPI stabilization. 相似文献
62.
Inside Cover: Stimuli‐Responsive Dual‐Color Photon Upconversion: A Singlet‐to‐Triplet Absorption Sensitizer in a Soft Luminescent Cyclophane (Angew. Chem. Int. Ed. 11/2018) 下载免费PDF全文
63.
Analysis of Cu segregation to oxide–metal interface of Ni‐based alloy in a metal‐dusting environment
Takashi Doi Kazuyuki Kitamura Yoshitaka Nishiyama Nobuo Otsuka Takeo Kudo Masugu Sato Eiji Ikenaga Shigenori Ueda Keisuke Kobayashi 《Surface and interface analysis : SIA》2008,40(10):1374-1381
Hard X‐ray photoelectron spectroscopy (HX‐PES) has been realized using high‐brilliance synchrotron radiation. High‐energy photon excitation enables us to probe photoelectrons with larger escape depth compared to conventional PES. This allows us to conduct, without destruction, a study of the embedded interface of materials as the oxide‐ metal interface. We apply HX‐PES to investigate for Cu segregation in the oxide–metal interface during metal‐dusting corrosion. The effective concentration of Cu in the segregation was estimated a few times higher than the bulk concentration. These results on the interface layer can explain the variation in the corrosion resistance. Copyright © 2008 John Wiley & Sons, Ltd. 相似文献
64.
We refine the computation of the d? ? ū flavor asymmetry in the proton sea with a complementary effort to reveal the dynamics of pion exchange in high-energy processes. In particular, we discuss the efficacy of pion exchange models to simultaneously describe leading neutron electroproduction at HERA along with the d? ? ū flavor asymmetry in the proton. A detailed \({\chi^{2}}\) analysis of the ZEUS and H1 data, when combined with constraints on the pion flux from Drell-Yan data, allows regions of applicability of one-pion exchange to be delineated. Based on the fit results, we also address a possible estimate for leading proton structure functions in upcoming tagged deep-inelastic scattering experiments at Jefferson Lab on the deuteron with forward protons. 相似文献
65.
Hiroshi Aoki Ken Hosoya Tomohisa Norisuye Nobuo Tanaka Daisuke Tokuda Norio Ishizuka Kazuki Nakanishi 《Journal of polymer science. Part A, Polymer chemistry》2006,44(2):949-958
An investigation was made of the gelation of dimethacrylate‐type crosslinking agents in view of an application for separation media. The study mainly centered on a crosslinking agent, glycerol dimethacrylate (GDMA), which is relatively hydrophilic because of a hydroxyl group in the middle of its structure. The gelation of GDMA was compared with that of other hydrophobic crosslinking agents such as ethylene glycol dimethacrylate and 1,6‐hexanediol dimethacrylate. The diluents used in the study were toluene, toluene with methanol, and cyclohexanol. The gelation was observed in real time with a charge coupled device camera and dynamic light scattering (DLS). Also, the separated dry gels were extensively characterized with scanning electron microscopy, BET (N2 absorption and desorption isotherm), and Fourier transform infrared. DLS analysis showed a stronger molecular interaction of GDMA gelation in toluene, whereas this interaction was much weaker in an alcoholic solvent such as toluene with methanol or cyclohexanol. This indicated that GDMA gelation might proceed through hydrogen bonding as well as a crosslinking reaction of vinyl groups. © 2005 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 44: 949–958, 2006 相似文献
66.
Yoshiyuki Watabe Takuya Kondo Hiroe Imai Masatoshi Morita Nobuo Tanaka Jun Haginaka Ken Hosoya 《Analytical sciences》2004,20(1):133-137
A new high-performance liquid chromatography (HPLC) method has been developed to detect ultra-low concentrations of bisphenol-A (BPA) (below 1 ng/L (ppt)) using column switching electrochemical detection (ECD). The results were superior to those obtained from manual pretreatment procedure with membrane stationary phase. BPA is inherently ubiquitous in the environment, including tools and solvents used for its analysis; to obtain meaningful results, therefore, the concentration of the overall BPA contamination must be below the detection limit for BPA using the analytical system. Therefore, purified water for preparing the standard BPA solution must be filtered with a hydrophobic membrane to suppress BPA background levels of contamination. In addition, we investigated methods for effectively preserving environmental water containing BPA. The addition of a small amount of ethylenediaminetetraacetic acid (EDTA) provided good recovery even after overnight storage. By employing these precautionary measures and procedures to reduce BPA contamination from the analytical procedure, we could accurately determine l(-10) ppt of BPA in environmental water samples using a column switching HPLC system. 相似文献
67.
In this paper we focus on the problem of identifying the index sets P(x):=i|xi>0, N(x):={i|Fi(x)>0 and C(x):=i|xi=Fi(x)=0} for a solution x of the monotone nonlinear complementarity problem NCP(F). The correct identification of these sets is important from both theoretical and practical points of view. Such an identification enables us to remove complementarity conditions from the NCP and locally reduce the NCP to a system which can be dealt with more easily. We present a new technique that utilizes a sequence generated by the proximal point algorithm (PPA). Using the superlinear convergence property of PPA, we show that the proposed technique can identify the correct index sets without assuming the nondegeneracy and the local uniqueness of the solution.This work was supported in part by a Grant-in-Aid for Scientific Research from the Ministry of Education, Science, Sports and Culture of Japan.Mathematics Subject Classification (2000): 90C33, 65K10 相似文献
68.
Fumiaki Watanabe Mitsuko Masutani Nobuo Kamada Hiroshi Suzuki Hitoshi Nakagama Takashi Sugimura Hirobumi Teraoka 《Proceedings of the Japan Academy. Series B, Physical and biological sciences》2004,80(6):248
One immediate cellular response to DNA damage is the polyADP-ribosylation reaction by poly(ADP-ribose) polymerase-1 (Parp-1). The importance of Parp-1 has been established in many cellular processes, such as the maintenance of genomic stability, DNA repair and cell-death induction. Here, we established Parp-1−/− mice of C57BL/6J congenic strain and characterized the role of Parp-1 in cell-cycle progression. In this study, we also improved a method to observe G0/G1 to S-phase transition of splenocytes and bone marrow cells prepared from mice. The cells were cultured and stimulated with mitogens (50 μM ionomycin/1 μM phorbol 12, 13-dibutyrate). We found that addition of a commercially available growth supportive reagent, BM Condimed RH1, greatly enhanced the transition of G0/G1 to the S-phase, which was determined by bromodeoxyuridine (BrdU) incorporation to DNA. Using this method, G0/G1 to the S-phase entry was measured using splenocytes derived from Parp-1−/−, Parp-1+/− and wild-type (Parp-1+/+) mice. DNA synthesis in Parp-1+/+ and Parp-1+/− splenocytes started from day 1 after addition of mitogens, whereas that in Parp-1−/− cells started from day 2. The peak of the S-phase was at day 2 in all genotypes and notably DNA synthesis in Parp-1−/− cells was approximately halved compared to Parp-1+/+ cells on day 2, 3 and 4. These results suggested that Parp-1 is involved in positive regulation of S-phase entry in quiescent mouse splenocytes. 相似文献
69.
70.
Tatsuhiko Kanmera Sannamu Lee Haruhiko Aoyagi Nobuo Izumiya 《Tetrahedron letters》1979,20(46):4483-4486
A series of cyclo (Δaminoacyl-L-Ala) () (Δ=α,β-dehydro) were prepared from cyclo(Gly-L-Ala) and corresponding aldehyde, and hydrogenated with Pd black in MeOH. Chiral inductions producing cyclo (L-aminoacyl-L-Ala) () from were 96–99% in the case of L-Aba (2-aminobutanoic acid), L-Val, L-Leu, and L-App (2-amino-5-phenylpentanoic acid) as an L-aminoacyl moiety in . Pure L-Leu, L-Aba, and L-App were synthesized in preparative scale from corresponding through asymmetric hydrogenation and acid-hydrolysis. 相似文献