以人工合成的多肽PGAT为底物,鉴定了人外周血淋巴细胞膜TPK。首次发现IATPD对该酶活性有较强的抑制作用,其IC50约为300μmol/L;改变其底物浓度,测定酶活性并应用Lineweaver-Burk双倒数作图法作图,结果表明,IATPD对该酶活性的抑制作用与ATP呈竞争性,与PGAT呈非竞争性。
In this paper, TPK activity from human peripheral blood lymphocyte membrane was measured using synthetic PGAT as substrate. The kinase activity was more strongly inhibited by a synthetic compound,1-isopropyl-6-amino-thieno (3,4-d) pyrimidine-2, 4-dione (IATPD); IC50 was about 300μmol/L. Lineweaver-Burk plots revealed that IATPD was competitively with ATP and noncompetitively with PGAT to inhibit the kinase activity.
张光毅,冯志民,魏涌,赵升皓,俞良莉,王礼琛. IATPD对淋巴细胞膜酪氨酸蛋白激酶的抑制作用[J].生物化学与生物物理进展,1992,19(3):190-194
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