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Proceedings for Annual Meeting of The Japanese Pharmacological Society最新文献

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Generation of genetically-encoded fluorescent sensors using molecular evolution and semi-rational molecular design 利用分子进化和半理性分子设计产生遗传编码荧光传感器
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.96.0_2-b-s14-1
Kitaguchi Tetsuya
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引用次数: 0
Effects of a novel hepatitis B antiviral drug in renal organic acid transporters 一种新型乙型肝炎抗病毒药物对肾有机酸转运体的影响
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.95.0_1-p-082
Misaki Ishibane, M. Kaneko, Shota Saito, Sangjon Pae, Shinpei Saito, Y. Reien, Yuri Hirayama, Hirofumi Hashimoto, N. Kuwata, H. Mitsuya, N. Anzai
In treatment of hepatitis B virus (HBV), it is usually difficult for us to control with emergence of drug resistance. As HBV often reactive after treatment was stopped, patients must keep it for long term. Recently, we have developed E-CFCP, as a candidate drug of HBV for patients with drug-resistant HBV. As it has high antiviral activity and the half-life also is longer, patients can take it in a once-weekly dosing. We expect that E-CFCP can greatly improve the quality of life of patients. However, effects of E-CFCP are unclear in renal. The aim of this study is to clarify the effects of E-CFCP in the kidney, especially organic acid transporter(Organic anion transporters:OATs, Organic cation transporter:OCT). We conducted cell viability studies using mouse-derived renal cortical cells (S2, CCD, cTAL) and uptake studies using radioisotopes to determine the effects of E-CFCP on the kidneys. In cell viability studies, E-CFCP has no cytotoxicity in all cell lines. We also examined the effect of drugs at high concentration using S2 cells. E-CFCP has no cytotoxicity even at high concentrations. In the substrate uptake assay, there was no inhibition of substrate uptake by E-CFCP, the transporter is not involved in the intracellular transport of E-CFCP and is unlikely to cause cytotoxicity. In conclusion, E-CFCP, a novel HBV antiviral drug, is unlikely to cause renal damage. It may be a novel great candidate drug of HBV for patients with drug-resistant HBV.
在乙型肝炎病毒(HBV)的治疗中,随着耐药性的出现,我们通常难以控制。由于HBV在停止治疗后经常发生反应,因此患者必须长期保持治疗。最近,我们开发了E-CFCP,作为耐药HBV患者的HBV候选药物。由于其抗病毒活性高,半衰期也较长,患者可以每周服用一次。我们期望E-CFCP能大大提高患者的生活质量。然而,E-CFCP对肾脏的影响尚不清楚。本研究的目的是阐明E-CFCP在肾脏中的作用,特别是有机酸转运体(有机阴离子转运体:OATs,有机阳离子转运体:OCT)。我们使用小鼠肾皮质细胞(S2、CCD、cTAL)进行了细胞活力研究,并使用放射性同位素进行了摄取研究,以确定E-CFCP对肾脏的影响。在细胞活力研究中,E-CFCP对所有细胞系均无细胞毒性。我们还利用S2细胞检测了高浓度药物的作用。即使在高浓度下,E-CFCP也没有细胞毒性。在底物摄取实验中,E-CFCP没有抑制底物摄取,转运体不参与E-CFCP的细胞内运输,不太可能引起细胞毒性。综上所述,E-CFCP是一种新型HBV抗病毒药物,不太可能引起肾脏损害。它可能是治疗耐药HBV患者的一种新的重要候选药物。
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引用次数: 0
Exploration of Nrf2-ARE pathway activators for the prevention and treatment of diseases Nrf2-ARE通路激活因子在疾病预防和治疗中的探索
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.96.0_4-b-s44-2
Yasuhiko Izumi
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引用次数: 0
From Discovery to Clinical application of PACAP PACAP从发现到临床应用
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.95.0_1-cl
A. Miyata
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引用次数: 0
Pharmacological action of ATP receptors and current status of related drug development ATP受体的药理作用及其药物开发现状
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.95.0_2-sl06
Kazuhide Inoue
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引用次数: 0
Doxorubicin did not affect the lysosomal acidification 阿霉素不影响溶酶体酸化
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.96.0_1-b-p-075
Takeya Sato, N. Toda, Masaki Saito, Masanori Yamauchi, Takaaki Abe
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引用次数: 0
Na+/Ca2+ exchanger type 1 functions as a “brake” of hyperactivation in hamster sperm. 1型Na+/Ca2+交换器在仓鼠精子中起着“刹车”的作用。
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.96.0_2-b-o03-3
L. Gen, Y. Ogura, Y. Ujihara, Fubito Toyama, Keitaro Hayashi, T. Fujita
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引用次数: 0
Purinergic regulation of mast cell function and allergic response via ionotropic P2X4 receptors 嘌呤能通过嗜离子性P2X4受体调控肥大细胞功能和过敏反应
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.96.0_1-b-s08-2
Kazuki Yoshida, Masa-aki Ito, I. Matsuoka
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引用次数: 0
Phospholipase C like protein PRIP1 PH-domain-containing liposomes enhance apoptotic cell death in cisplatin resistant breast cancer cells 磷脂酶C样蛋白PRIP1含ph结构域脂质体促进顺铂耐药乳腺癌细胞的凋亡细胞死亡
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.96.0_1-b-p-076
Asano Satoshi, Y. Ago, T. Kanematsu
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引用次数: 0
Three-dimensional structural analysis of pharmacokinetics-related membrane protein P-glycoprotein using cryo-electron microscopy 用冷冻电镜分析药代动力学相关膜蛋白p -糖蛋白的三维结构
Pub Date : 2022-01-01 DOI: 10.1254/jpssuppl.96.0_1-b-ss05-1
Hamaguchi Norie, N. Adachi, T. Moriya, M. Kawasaki, Kenji Yasuda, T. Senda, Satoshi Oagasawara, T. Murata
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引用次数: 0
期刊
Proceedings for Annual Meeting of The Japanese Pharmacological Society
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