Morita H, Nagashima S, Takeya K, Itokawa H
Department of Pharmacognosy, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Japan.
Chem Pharm Bull (Tokyo). 1995 Aug;43(8):1395-7. doi: 10.1248/cpb.43.1395.
Conformational analysis of antitumor cyclic pentapeptides, astins A (1) and C (3), was made by a combination of NMR and computational techniques. These results indicated that the backbone conformations of 1 and 3, with lower activity than astin B (2), were different from that of 2. The backbone conformation together with a cis 3,4-dichlorinated proline residue was considered to play an important role in the antitumor activities of astins.
通过核磁共振(NMR)和计算技术相结合的方法,对抗肿瘤环五肽阿斯汀A(1)和C(3)进行了构象分析。这些结果表明,活性低于阿斯汀B(2)的1和3的主链构象与2不同。主链构象以及顺式3,4 - 二氯脯氨酸残基被认为在阿斯汀的抗肿瘤活性中起重要作用。