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961.
Pattaporn Jaikhan Benjaporn Buranrat Yukihiro Itoh Jiranan Chotitumnavee Takashi Kurohara Takayoshi Suzuki 《Bioorganic & medicinal chemistry letters》2019,29(10):1173-1176
Fe(II)/α-ketoglutarate-dependent lysine demethylases (KDMs) are attractive drug targets for several diseases including cancer. In this study, we designed and screened ortho-substituted anilides that are expected to function as Fe(II) chelators, and identified ortho-hydroxy anilide as a novel scaffold for KDM5A inhibitors. Treatment of human lung cancer A549 cells with a prodrug form of 4-carboxy-2-hydroxy-formanilide (9c) increased trimethylated lysine 4 on histone H3 level, suggesting KDM5 inhibition in the cells. 相似文献
962.
Toshihiro Hamajima Fumie Takahashi Koji Kato Yukihito Sugano Susumu Yamaki Daisuke Suzuki Ayako Moritomo Satoshi Kubo Koji Nakamura Kaoru Yamagami Koji Yokoo Hidehiko Fukahori 《Bioorganic & medicinal chemistry》2019,27(6):1056-1064
Chemical optimization of the 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine (THPP) scaffold was conducted with a focus on cellular potency while maintaining high selectivity against PI3K isoforms. Compound 11f was identified as a potent, highly selective and orally available PI3Kδ inhibitor. In addition, 11f exhibited efficacy in an in vivo antibody production model. The desirable drug-like properties and in vivo efficacy of 11f suggest its potential as a drug candidate for the treatment of autoimmune diseases and leukocyte malignancies. 相似文献
963.
Susan K. Boehlein Peng Liu Ashley Webster Camila Ribeiro Masaharu Suzuki Shan Wu Jiahn‐Chou Guan Jon D. Stewart William F. Tracy A. Mark Settles Donald R. McCarty Karen E. Koch Larkin C. Hannah Tracie A. Hennen‐Bierwagen Alan M. Myers 《The Plant journal : for cell and molecular biology》2019,99(1):23-40
964.
We are developing techniques to restore coral populations by enhancing larval supply using “artificial spawning hotspots” that aggregate conspecific adult corals. However, no data were available regarding how natural larval supply from wild coral populations is influenced by fertilization rate and how this is in turn affected by local population density and genetic diversity. Therefore, we assessed population density and genetic diversity of a wild, arborescent coral, Acropora yongei, and compared these parameters with those of an artificially established A. yongei population in the field. The population density of wild arborescent corals was only 0.27% of that in the artificial population, even in a high‐coverage area. Genetic diversity was also low in the wild population compared with the artificial population, and approximately 10% of all wild colonies were clones. Based on these results, the larval supply in the artificial population was estimated to be at least 1,400 times higher than that in wild A. yongei populations for the same area of adult population. 相似文献
965.
Takashi Yazawa Yoshitaka Imamichi Koh‐ichi Yuhki Junsuke Uwada Daisuke Mikami Masayuki Shimada Kaoru Miyamoto Takeshi Kitano Satoru Takahashi Toshio Sekiguchi Nobuo Suzuki Md. Rafiqul Islam Khan Fumitaka Ushikubi Akihiro Umezawa Takanobu Taniguchi 《Molecular reproduction and development》2019,86(7):786-797
966.
967.
Participation of caspase-3-like protease in oxidation-induced impairment of erythrocyte membrane properties 总被引:1,自引:0,他引:1
Erythrocytes are very susceptible to oxidative stress, having a high content of intracellular oxygen and hemoglobin. In the present study, exposure to oxidative stress resulted in a significant impairment of erythrocyte membrane functions, such as deformability and anion exchange. Band 3 protein, also known as anion exchanger-1, plays an important role in these two functions. We show that oxidative stress activated caspase-3 inside the erythrocytes, which resulted in band 3 protein cleavage. Interestingly, inhibition of the caspase-3 with its specific inhibitor not only suppressed the digestion of band 3 protein, but also blunted the functional damage to erythrocytes, such as deformability and anion exchange, without changing the level of peroxidation of membrane lipids. These results provide experimental evidence that activation of caspase-3 plays an important role in the oxidative stress-induced impairment of membrane functions of erythrocytes. 相似文献
968.
Therian mammals (marsupials and eutherians) rely on a placenta for embryo survival. All mammals have a yolk sac, but while both chorio-allantoic and chorio-vitelline (yolk sac) placentation can occur, most marsupials only develop a yolk sac placenta. Insulin (INS) is unusual in that it is the only gene that is imprinted exclusively in the yolk sac placenta. Marsupials, therefore, provide a unique opportunity to examine the conservation of INS imprinting in mammalian yolk sac placentation. Marsupial INS was cloned and its imprint status in the yolk sac placenta of the tammar wallaby, Macropus eugenii, examined. In two informative individuals of the eight that showed imprinting, INS was paternally expressed. INS protein was restricted to the yolk sac endoderm, while insulin receptor, IR, protein was additionally expressed in the trophoblast. INS protein increased during late gestation up to 2 days before birth, but was low the day before and on the day of birth. The conservation of imprinted expression of insulin in the yolk sac placenta of divergent mammalian species suggests that it is of critical importance in the yolk sac placenta. The restriction of imprinting to the yolk sac suggests that imprinting of INS evolved in the chorio-vitelline placenta independently of other tissues in the therian ancestor of marsupials and eutherians. 相似文献
969.
970.
The tiger pufferfish (fugu), Takifugu rubripes, is a model fish that has had its genome entirely sequenced. By performing genomewide linkage analyses, we show that the sex of fugu is determined by a single chromosomal region on linkage group 19 in an XX-XY system. 相似文献