Kawasaki K, Murakami T, Namikawa M, Mizuta T, Iwai Y, Yamashiro Y, Hama T, Yamamoto S, Mayumi T
Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Japan.
Chem Pharm Bull (Tokyo). 1994 Apr;42(4):917-21. doi: 10.1248/cpb.42.917.
Laminin-related peptides, Tyr-Ile-Gly-Ser-Arg analogs, were prepared and their inhibitory effects on experimental metastasis were examined. Of the amino acids in the Tyr-Ile-Gly-Ser-Arg sequence, L-Arg was very important and Ile was not essential for the inhibitory effect. To obtain a potent inhibitor of metastasis, hybrids of Tyr-Ile-Gly-Ser-Arg-Gly and 2 types of poly(ethylene glycol) were prepared. The inhibitory effects of the hybrids were more potent than that of Tyr-Ile-Gly-Ser-Arg-Gly.
制备了层粘连蛋白相关肽,即酪氨酸 - 异亮氨酸 - 甘氨酸 - 丝氨酸 - 精氨酸类似物,并检测了它们对实验性转移的抑制作用。在酪氨酸 - 异亮氨酸 - 甘氨酸 - 丝氨酸 - 精氨酸序列中的氨基酸中,L - 精氨酸非常重要,而异亮氨酸对抑制作用并非必不可少。为了获得一种有效的转移抑制剂,制备了酪氨酸 - 异亮氨酸 - 甘氨酸 - 丝氨酸 - 精氨酸 - 甘氨酸与两种聚乙二醇的杂化物。这些杂化物的抑制作用比酪氨酸 - 异亮氨酸 - 甘氨酸 - 丝氨酸 - 精氨酸 - 甘氨酸更强。