Shieh H M, Campbell D, Folkers K
Biochem Biophys Res Commun. 1984 Jul 18;122(1):21-7. doi: 10.1016/0006-291x(84)90433-9.
To synthesize peptidic derivatives of polyamines, sequential reactions were designed for the polyfunctional peptides and polyfunctional amines which utilize specific protection and deprotection. Utilizing these reactions, a thymic nonapeptide, a lymphocyte-differentiating hormone, was coupled with spermidine and spermine to yield, respectively: Glp-Ala-Lys-Ser-Gln-Gly-Gly-Ser-Asn-NH(CH2)3NH(CH2)4NH2; Glp-Ala-Lys-Ser-Gln-Gly-Gly-Ser-Asn-NH(CH2)3NH-(CH2)4NH(CH2) 3NH2. Both conjugates inhibited rather than stimulated incorporation of [3H]-thymidine into DNA at levels 20-fold that of spermine. This activity is less than that based on the percent of the spermine moeity (ca. 20%) in the conjugate.
为了合成多胺的肽衍生物，针对利用特定保护和脱保护的多官能肽和多官能胺设计了连续反应。利用这些反应，将一种胸腺九肽（一种淋巴细胞分化激素）与亚精胺和精胺偶联，分别得到：Glp-Ala-Lys-Ser-Gln-Gly-Gly-Ser-Asn-NH(CH2)3NH(CH2)4NH2；Glp-Ala-Lys-Ser-Gln-Gly-Gly-Ser-Asn-NH(CH2)3NH-(CH2)4NH(CH2) 3NH2。两种缀合物均抑制而非刺激[3H]-胸腺嘧啶核苷掺入DNA，其水平是精胺的20倍。该活性低于基于缀合物中精胺部分（约20%）的活性。
