图1. 激酶催化的ATP介导的磷酸化反应过程。
图1. FDA批准小分子激酶抑制剂药物年份数量图。
图2. 部分FDA批准的激酶抑制剂药物分子结构。
图3. 激酶抑制剂常见的芳香杂环结构。
[1] Manning, G. et al. The protein kinase complement of the human genome. Science. 2002, 298, 1912–1934.
[2] Cohen, P. The regulation of protein function by multisite phosphorylation — a 25 year update. Trends Biochem. Sci. 2000, 25, 596–601.
[3] Manning, G., et al. The protein kinase complement of the human genome. Science. 2002, 298, 1912–1934.
[4] Muller, S. et al. The ins and outs of selective kinase inhibitor development. Nat. Chem. Biol. 2015, 11, 818–821.
[5] Roskoski, R. Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update. Pharmacol Res. 2020, 152, 104609.
[6] Green, K. N. et al. To Kill a Microglia: A Case for CSF1R Inhibitors. Trends in Immunology. 2020, 41, 771–784.
[7] Imatinib Mesylate. The American Society of Health-System Pharmacists.
[8] Wu, P. et al. FDA-approved small-molecule kinase inhibitors. Trends Pharmacol Sci. 2015, 36, 422-439.
[9] Keating, J. A. et al. Phosphorylation events during viral infections provide potential therapeutic targets. Rev. Med. Virol. 2012, 22, 166–181.
[10] García-Cárceles, J. et al. Kinase Inhibitors as Underexplored Antiviral Agents. J Med Chem. 2022, 65, 935–954.
[11] Blake, S. et al. The Src/ABL kinase inhibitor dasatinib (BMS-354825) inhibits function of normal human T-lymphocytes in vitro. Clin. Immunol. 2008, 127, 330–339.
[12] Naik, R. R. et al. Kinase Inhibitors as Potential Therapeutic Agents in the Treatment of COVID-19. Front. Pharmacol. 2022, 13, 806568.
2024-08-17
2024-09-02
2024-08-09
2024-08-06
2024-08-19
2024-08-15
2024-08-28
本文的目的是为了探讨注射用甲苯磺酸奥马环素的无菌方法开发及验证。通过采用薄膜过滤法,使用1mol·L-1硫酸镁溶液对样品及所用培养基进行处理,pH 7.0 氯化钠蛋白胨缓冲液(含 0.1% 组氨酸、0.3% 卵磷脂和 3% 吐温 80)进行冲洗,有效地消除了样品的抑菌性。得出的结论为采用 1 mol·L-1 硫酸镁溶液及 pH 7.0 氯化钠蛋白胨缓冲液(含 0.1% 组氨酸、0.3% 卵磷脂和 3% 吐温 80)可以有效地消除注射用甲苯磺酸奥马环素的抑菌性能,可以将该方法用于注射用甲苯磺酸奥马环素的无菌方法验证。
作者:印萍
评论
加载更多