Kyle D J, Green L M, Blake P R, Smithwick D, Summers M F
Nova Pharmaceutical Corporation, Baltimore, MD 21224.
Pept Res. 1992 Jul-Aug;5(4):206-9.
Ethers of cis or trans D-4-hydroxyproline (Hype), adjacent to octahydroindole-carboxylic acid (Oic), introduce a beta-turn into the backbone of peptides when positioned respectively at the i+1 and i+2 position of the turn. This is confirmed by NMR experiments performed on a model tetrapeptide in water. Synthetic alteration of the ether group allows simple probing of the steric limits and electrostatic potential of a receptor binding site, a technique applied successfully to the bradykinin receptor.
与八氢吲哚 - 羧酸（Oic）相邻的顺式或反式D - 4 - 羟基脯氨酸（Hype）醚，当分别位于转角的i + 1和i + 2位置时，会在肽的主链中引入一个β - 转角。这通过在水中对模型四肽进行的核磁共振实验得到证实。醚基团的合成改变允许对受体结合位点的空间限制和静电势进行简单探测，该技术已成功应用于缓激肽受体。
