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71.
Dr. Daisuke Fujiwara Kousuke Mihara Ryo Takayama Yusuke Nakamura Prof. Mitsuhiro Ueda Prof. Takeshi Tsumuraya Prof. Ikuo Fujii 《Chembiochem : a European journal of chemical biology》2021,22(24):3406-3409
Conformationally constrained peptides hold promise as molecular tools in chemical biology and as a new modality in drug discovery. The construction and screening of a target-focused library could be a promising approach for the generation of de novo ligands or inhibitors against target proteins. Here, we have prepared a protein kinase-focused library by chemically modifying helix-loop-helix (HLH) peptides displayed on phage and subsequently tethered to adenosine. The library was screened against aurora kinase A (AurA). The selected HLH peptide Bip - 3 retained the α-helical structure and bound to AurA with a KD value of 13.7 μM. Bip - 3 and the adenosine-tethered peptide Bip - 3 - Adc provided IC50 values of 103 μM and 7.7 μM, respectively, suggesting that Bip - 3 - Adc bivalently inhibited AurA. In addition, the selectivity of Bip - 3 - Adc to several protein kinases was tested, and was highest against AurA. These results demonstrate that chemical modification can enable the construction of a kinase-focused library of phage-displayed HLH peptides. 相似文献
72.
Summary Spontaneous copolymerizations of cyclic acyl phosphonite (SPO) and phosphite (SPI) with an electron-deficient vinyl monomer
such as methyl acrylate (MA), methyl vinyl ketone (MVK), and acrolein (AL), gave the corresponding alternating copolymers.
These copolymerizations took place without added initiator and proceeded through zwitterion intermediates. Copolymer structures
1a, 1b, 2 and 3 have been established, all of which were derived in a regiospecific manner of ambident anions. The scheme of the copolymerizations
is presented. 相似文献
73.
Summary The ring-opening polymerization of 2-phenyl-1,3,-6,2-trioxaphosphocane (4), an eight-membered cyclic phosphonite, has been investigated. Cationic initiators of PhCH2-Cl and MeOTf gave polymers, whereas anionic and radical initiators did not yield polymer. The structure of polymer was examined by IR, 1H, 31P, and 31C NMR spectroscopy of polymers and elemental analysis as well as the alkaline hydrolysis products. The polymer consisted of two different units, i.e., the major part is the normal phosphinate structure 5 and the minor part is the isomerized unit 6 in 7% with PhCH2Cl initiation and in 34% with MeOTf initiator. The difference in nature of propagating species from these two initiators are discussed in connection with their reactivities.On leave from the Institute of Chemistry, Academia Sinica, Beijing, China 相似文献
74.
Summary The ring-opening polymerization of deoxophostone 5, a five-membered cyclic phosphinite, has been studied. Some cationic initiators gave polymer whereas anionic and radical initiators as well as metal chloride (Lewis acid) catalysts did not yield polymer. The polymer consisted of a phosphine oxide repeating unit 6. The polymerization proceeded via the Arbuzov-type reaction. The reduction of polymer 6 with a HSiCl3/Et3N system gave polyphosphine 7. 相似文献
75.
Takashi Mitamura Hiroyuki Ogino Hidehiko Kobayashi Toshiyuki Mori Hiroshi Yamamura 《Journal of the American Ceramic Society》1993,76(8):2127-2128
Preparation of BaLa2 O4 , Ba3 ,Y4 O9 , Ba ,In2 O5 , and Ba3 Ga2 O6 powders and their sintering were investigated in Ar or air. These sintered bodies with perovskite-related structure were synthesized by reaction sintering, using mixed powders in the atomic ratios of Ba/La = 1, Ba/Y = 0.75, Ba/In = 1, and Ba/Ga = 1.5. The order-disorder transition temperatures of the BaLa2 O4 , Ba3 Y4 O9 , Ba2 In2 O5 , and Ba3 Ga2 O6 sintered bodies were 270°, 350°, 880°, and 123Oo C, respectively. It was found that the temperatures were influenced by the ionic radius of cations in B sites, and the transition temperatures decreased with increasing ionic radius. 相似文献
76.
Summary Glow discharge polymerizations of allyltrimethylsilane (ATMS) and trimethylvinyloxysilane (TMVOS) were investigated by elemental analysis and infrared spectroscopy. The formed polymers were far different in elemental composition from the starting materials, and possessed high carbon and hydrogen contents. There was less difference in an infrared-spectral sense between the two polymers from ATMS and TMVOS. A polymer-forming process in a discharge state is discussed. 相似文献
77.
78.
Motoi Takahashi Toshiyuki Mori Fei Ye Ajayan Vinu Hidehiko Kobayashi John Drennan 《Journal of the American Ceramic Society》2007,90(4):1291-1294
A Pt on nano-sized CeO2 particles that in turn are supported on carbon black (CB) was synthesized using the co-impregnation method. This potential anode material for fuel cell applications was synthesized in a stepwise process. The pure CeO2 was synthesized using an ammonium carbonate precipitation method, and the Pt particles dispersed on the CeO2 in such a way that a uniform dispersion with the CB was obtained (Pt–CeO2 /CB). The electrochemical activity of the methanol (CH3 OH) oxidation reaction on the Pt–CeO2 /CB was investigated using cyclic voltammetry and chronoamperometry experimentation. The onset potential of CH3 OH oxidation reaction on the Pt–CeO2 /CB anode was shifted to a lower potential as compared with that on commercially available Pt–Ru/carbon (C) alloy anode. In addition, the activation energy of the Pt–CeO2 /CB anode was much lower than that of the Pt–Ru/C alloy anode. Moreover, the current density of the Pt–CeO2 /CB anode was much higher than that of the Pt–Ru/C alloy anode at temperatures between 28° and 60°C. These results suggest that the anode performance of the Pt–CeO2 /CB anode at the operating temperature of typical fuel cells (80°C) is superior to that of the more usual Pt–Ru/C alloy anode. Importantly, the rare metal, Ru, is not required in the present anode material and the amount of Pt required is also significantly reduced. As a consequence, we report a promising candidate Pt–CeO2 /CB composite anode for application in the development of direct methanol fuel cells. 相似文献
79.
A Sm(III) exchanged NaY zeolite prepared from aqueous SmCl3 was modified with various amounts of fluorine using NH4F. These fluorinated zeolites exhibit enhanced catalytic activity for the dealkylation of cumene. The evaluation of acid sites by infrared spectroscopy and pyridine adsorption was correlated with fluorine content. 相似文献
80.
Shigeki Habaue Momoko AsaiMasatake Morita Yoshio OkamotoHiroshi Uyama Shiro Kobayashi 《Polymer》2003,44(18):5195-5200
α-Methylenemacrolides having various groups, such as aromatic, ether, and amine, were enzymatically, anionically, and radically polymerized. The polymerization with the lipase catalyst successfully afforded polymers only through the ring-opening process, whereas the vinyl polymerizations selectively proceeded by using anionic and radical initiators. The polyesters obtained by the enzymatic polymerization have a polymerizable methacrylic methylene group in the main-chain, in addition to the aromatic and polar groups, and were further radically polymerized to quantitatively produce a cross-linked polymer gel. 相似文献