Sugase Kenji, Horikawa Manabu, Sugiyama Masako, Ishiguro Masaji
Suntory Institute for Bioorganic Research and Daiichi Suntory Biomedical Research Co., Ltd, Shimamoto, Mishima 618-8503, Japan.
J Med Chem. 2004 Jan 15;47(2):489-92. doi: 10.1021/jm030232j.
Compounds (2S,4S)- and (2S,4R)-4-(2'-guanidinoethyl)proline have been synthesized as a conformationally restricted arginine. Their backbones fit the i + 1 position in a turn, and the side chains are restricted compared to that of arginine. These analogues were incorporated into mini atrial natriuretic polypeptide, which has an important turnlike conformation at Gly(6)-Arg(7)()-Met(8)-Asp(9). Structural analysis revealed that the size of the conformational space of Arg(7) on binding to the receptor was approximately one-third of the entire conformational space.
化合物(2S,4S)-和(2S,4R)-4-(2'-胍基乙基)脯氨酸已被合成为一种构象受限的精氨酸。它们的主链适合于转角处的i + 1位置，并且与精氨酸相比，侧链受到限制。这些类似物被并入微型心房利钠多肽中，该多肽在Gly(6)-Arg(7)-Met(8)-Asp(9)处具有重要的转角样构象。结构分析表明，Arg(7)与受体结合时构象空间的大小约为整个构象空间的三分之一。
