肌醇1,4,5-三磷酸类似物1-磷酸处的疏水修饰增强受体结合。
Hydrophobic modifications at 1-phosphate of inositol 1,4,5-trisphosphate analogues enhance receptor binding.
作者信息
Nakanishi Waka, Kikuchi Kazuya, Inoue Takanari, Hirose Kenzo, Iino Masamitsu, Nagano Tetsuo
机构信息
Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan.
出版信息
Bioorg Med Chem Lett. 2002 Mar 25;12(6):911-3. doi: 10.1016/s0960-894x(02)00044-6.
Abstract
Inositol 1,4,5-trisphosphate (IP(3)) analogues were synthesized in order to investigate the importance of the environment of 1-phosphate of IP(3) for strong binding to the IP(3) receptor. Our results show that hydrophobic modifications of the 1-phosphate moiety enhance the binding affinity, with considerable latitude of substituent structure.
摘要
为了研究1,4,5-三磷酸肌醇（IP(3)）1-磷酸基团的环境对于与IP(3)受体紧密结合的重要性，合成了IP(3)类似物。我们的结果表明，1-磷酸基团部分的疏水修饰增强了结合亲和力，且取代基结构具有相当大的自由度。
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