抗癌多肽体

摘要

圆饼状结构体含有3对内部二硫键形成有内环和外环的圆饼形状的构造。这里探索到圆饼状结构体的内环上存在两个抗毛细血管内皮细胞活性区,其活性能够转达到相对应的多肽体上。由此发明人发现了两个具有抑制内皮细胞生长活性的微小多肽体。它们的长度分别仅为7和10个氨基酸。这些多肽体易于被制造和大量生产,是治疗肿瘤和防治糖尿病所致失明等疾病的新的血管抑制素。

主权项

具有抗毛细血管内皮细胞增生的两个微小多肽体D肽(10个氨基酸)和e肽(仅含7个氨基酸)的制造及其应用于治疗癌症和防治糖尿病诱发性失明或其它与血管增生有关的疾病。1. 多肽体D肽的组成组成为：X1-Arg-Asn-Pro-Asp-Gly-Asp-Ala-Z1-Pro-Trp-X2。Z1是一个带正电荷的氨基酸如赖氨酸或精氨酸等。X1是醋酸基或其它N-末端保护基如formyl，propionyl，pivaloyl，2-chloroacetyl，2-bromoacetyl，trifluoroacetyl，trichloroacetyl，phthalyl，o-nitro-phenoxyacetyl，benzyloxy-carbonyl，p-chlorobenzyl-oxycarbonyl，benzyloxy-carbonyl，p-chlorobenzyloxycarbonyl，p-bromobenzyloxycarbonyl，p-nitro-benzyloxycarbonyl，p-methoxybenzyloxycarbonyl，2-nitrobenzyloxycarbonyl，2-nitro-4，5-dimethoxybenzyloxy-carbonyl，2，4-dimethoxybenzyloxycarbonyl，4-methoxy-benzyloxy-carbonyl，1-(p-biphenylyl)-1-methylethoxycarbonyl，benzhydryloxy-carbonyl，t-butyloxycarbonyl，diisopropylmethoxycarbonyl，isopropyloxy-carbonyl，ethoxycarbonyl，methoxycarbonyl等。X2是氨基，乙醇氨基或其它C-末端保护基如phenethyl，alkoxy-benzyl，alkanoyloxyalkyl acetoxymethyl，butyryl-oxymethyl，1-methyl-1-(propionyloxy)-1-ethyl，pivaloyloxymethyl，cyclopropylcarbonyloxymethyl，cyclobutylcarbonyloxymethyl，cyclopentylcarbonyloxymethyl，cyclohexyl-carbonyloxymethyl，benzoyloxymethyl，benzoyloxyethyl，benzylcarbonyl-oxymethyl，2-benzylcarbonyloxyethyl，methoxycarbonylmethyl，cyclohexyl-oxycarbonylmethyl，1-methoxycarbonyl-1-ethyl，methoxycarbonyloxymethyl，1-ethoxycarbonyloxy-1-ethyl，1-cyclohexyloxycarbonyloxy-1-ethyl，t-butyl-oxycarbonylamino-meoyl 2-(phenoxycarbonyloxy)ethyl，2-(5-indanyloxy-carbonyloxy)ethyl，2-(1-methoxy-2-methylpropan-2-oyloxy)ethyl，2-(bcnzyl-oxycarbonyloxy)ethyl等。