Sivanandaiah K M, Babu V V, Shankaramma S C, Lakshmana M, Babu R, Arif M A, Kumar M
Department of Studies in Chemistry, Bangalore University, Central College, India.
Indian J Exp Biol. 1996 Jul;34(7):658-62.
The synthetic laminin pentapeptide amide fragment (LF), Tyr-Ile-Gly-Ser-Arg-NH2 corresponding to a part of B1 chain of the glycoprotein, laminin, and six of its analogues having structural modifications at positions 1, 3 and 4 were synthesized by solid phase method employing mainly 9-fluorenylmethoxycarbonyl-amino acid trichlorophenyl esters as coupling agents and Merrifield resin as the solid support. Their biological activities were studied in vivo by lung tumor colonization assay and in vitro by cell adhesion assay. The activity of synthetic LF was found to correlate with the earlier reported results in both in vivo and in vitro assays. Among the analogues made, [Tyr4] LF and [Thr4]LF were found to inhibit the lung tumor colonies more efficiently than LF itself in the in vivo assay whereas [D- Ser4]LF exhibited almost the same inhibition as LF.
合成层粘连蛋白五肽酰胺片段（LF），即对应糖蛋白层粘连蛋白B1链一部分的Tyr-Ile-Gly-Ser-Arg-NH2，以及在第1、3和4位具有结构修饰的其六种类似物，采用主要以9-芴甲氧羰基 - 氨基酸三氯苯基酯为偶联剂、Merrifield树脂为固相载体的固相法合成。通过肺肿瘤定植试验在体内研究它们的生物学活性，并通过细胞粘附试验在体外进行研究。发现在体内和体外试验中，合成LF的活性与早期报道的结果相关。在所制备的类似物中，在体内试验中发现[ Tyr4]LF和[Thr4]LF比LF本身更有效地抑制肺肿瘤集落，而[D-Ser4]LF表现出与LF几乎相同的抑制作用。
