Bumpus F M
Fed Proc. 1977 Jul;36(8):2128-32.
From the myotropic and vasopressor activities of the numerous analogs of angiotensin II, it has been determined that the phenyl group of position 8 possesses the information for biologic response while the aromatic side groups in positions 4 and 6, the guanido group in position 2 and the C-terminal carboxyl are involved in binding to the receptor site. Removal of a side group of the C-terminal phenyalanine yields peptides that bind to the receptor. While many of these have low agonist properties, all have antagonist properties. Modifications in the aromatic side groups affect conformation of the octapeptide. This change may relate to receptor binding but sufficient data are not yet available to determine a correlation pattern. A proposed conformation for angiotensin is given as well as an artist's concept of angiotensin II binding to its membrane receptor utilizing the groups known to be involved in binding. Both angiotensin II and III [des-Asp] angiotensin II stimulate the biosynthesis and release of aldosterone from adrenal glomerulosa cells. Sufficient data are not yet available to determine whether the conversion of angiotensin II to angiotensin III is neccessary for the steroidogenesis activity.
从众多血管紧张素II类似物的亲肌性和血管加压活性可知，8位的苯基具有生物反应信息，而4位和6位的芳香侧基、2位的胍基以及C末端羧基参与与受体位点的结合。去除C末端苯丙氨酸的一个侧基会产生与受体结合的肽。虽然其中许多具有低激动剂特性，但都具有拮抗剂特性。芳香侧基的修饰会影响八肽的构象。这种变化可能与受体结合有关，但尚无足够数据来确定相关模式。给出了血管紧张素的一种推测构象以及血管紧张素II利用已知参与结合的基团与其膜受体结合的示意图。血管紧张素II和III [去天冬氨酸]血管紧张素II都能刺激肾上腺球状带细胞中醛固酮的生物合成和释放。尚无足够数据来确定血管紧张素II向血管紧张素III的转化对于类固醇生成活性是否必要。
