Study on Biomaterials for Drug Delivery Sysytem Based on Dynamic Structural Change of Molecular Assembly of Elastin Peptides

根据具有自组装性质的重复五肽序列Val-Pro-Gly-Val-Gly合成了具有自组装性质的高聚物、可被蛋白激酶磷酸化的肽arg - gly - tyrr - ser - leu - gly、可将Asn残基转化为Asp残基的肽Gly-Ser-Asn-His-Gly和Gly-Arg-Asn-Thr-Gly。arg - gly - tyrr - ser - leu - gly被环AMP依赖性蛋白激酶磷酸化。Gly-Ser-Asn-His-Gly和gly - arg - asn - sr - gly的半衰期分别为6天和28天。<1996>Poly [15 (Val-Pro-Gly-Val-Gly), (Arg-Gly-Tyr-Ser-Leu-Gly)]由指定的摩尔比组成。该聚合物经环AMP依赖性蛋白激酶在30℃下磷酸化24小时。研究了合成的磷酸化聚合物[15 (Val-Pro-Gly-Val-Gly), (Arg-Gly-Tyr-Ser (PO_4^<2->) - leu - gly)]的自组装性能。磷酸化聚合物的反温度转变温度（Tm）被转移到更高的温度，从而产生14个温度转移。将磷酸化的聚合物与碱性磷酸酶在30℃下孵育4小时，得到去磷酸化的聚物[15 (Val-Pro-Gly-Val-Gly), (Arg-Gly-Tyr-Ser-Leu-Gly)]。Tm被转移到较低的温度，从而产生13个tc3的位移。这一结果表明磷酸化聚合物完全去磷酸化。

<1995>A high polymer based on the repeating pentapeptide sequence Val-Pro-Gly-Val-Gly which has the property of salf-assembly, a peptide Arg-Gly-Tyr-Ser-Leu-Gly which can be phosphorylated by protein kinase, and two peptides Gly-Ser-Asn-His-Gly and Gly-Arg-Asn-Thr-Gly in which Asn residue can be converted to Asp residue, were synthesized. Arg-Gly-Tyr-Ser-Leu-Gly was phosphorylated by cyclic AMP dpendent protein kinase. The half-lives for Asn-Asp conversion were 6 days and 28 days for Gly-Ser-Asn-His-Gly and Gly-Arg-Asn-Thr-Gly.<1996>Poly [15 (Val-Pro-Gly-Val-Gly), (Arg-Gly-Tyr-Ser-Leu-Gly)] which consists of the indicated molar ratios was synthesized. This polymer was phosphorylated by cyclic AMP dependent protein kinase for 24 hr at 30ﾟC.The resulting phosphorylated polymer poly [15 (Val-Pro-Gly-Val-Gly), (Arg-Gly-Tyr-Ser (PO_4^<2->) -Leu-Gly)] was studied for self-assembly. The temperature for the inverse temperature transition (Tm) of the phosphorylated polymer was shifted to higher temperature giving a shift of 14ﾟC.The phosphorylated polymer was incubated with alkaline phosphatase for 4 hr at 30ﾟC to yield a dephosphorylated poly [15 (Val-Pro-Gly-Val-Gly), (Arg-Gly-Tyr-Ser-Leu-Gly)]. Tm was shifted to lower temperature giving a shift of 13ﾟC.This result indicated complete dephosphorylation of phosphorylated polymer.