Van Nispen J W, Tesser G I, Nivard R J
Int J Pept Protein Res. 1977;9(3):193-202. doi: 10.1111/j.1399-3011.1977.tb03481.x.
Two new ACTH-analogues, an octadecapeptide amide and a tetracosapeptide containing the lower homologue of arginine (norarginine) in position 8, have been synthesized by the generally accepted method. Special attention was paid to the synthesis of the required tetrapeptide representing the 7-10 sequence, which was obtained either by direct introduction of L-nitronorarginine or by amidination of the gamma-amino function in a protected peptide containing alpha, gamma-diaminobutyric acid. Biological activity determination showed that the shortening e arginine side chain in position 8 results in the formation of active ACTH-analogues.
通过普遍认可的方法合成了两种新的促肾上腺皮质激素(ACTH)类似物,一种是十八肽酰胺,另一种是在第8位含有精氨酸(正精氨酸)较低同系物的二十四肽。特别关注了代表7-10序列的所需四肽的合成,该四肽可通过直接引入L-硝基正精氨酸或通过对含有α,γ-二氨基丁酸的受保护肽中的γ-氨基功能进行酰胺化来获得。生物活性测定表明,缩短第8位的精氨酸侧链会导致形成活性ACTH类似物。