Investigation of binding proteins for anti-platelet agent K-134 by Drug-Western method.
Investigation of binding proteins for anti-platelet agent K-134 by Drug-Western method.
复制标题
通过 Drug-Western 方法研究抗血小板剂 K-134 的结合蛋白。
DOI：
10.1016/j.bbrc.2006.12.172
复制
发表时间：
2007
影响因子：
3.1
通讯作者：
H. Hidaka
中科院分区：
文献类型：
--
作者：
M. Ikenoya;T. Doi;T. Miura;K. Sawanobori;M. Nishio;H. Hidaka
K-134（（-）-6-[3-[3-环丙基-3-[（1 R，2 R）-2-羟基环己基]脲基]-丙氧基]-2（1H）-喹啉酮）是一种具有抗血小板增生活性的新型抗血小板药物。我们以前发现K-134是一种有效的磷酸二酯酶-3（PDE 3）抑制剂。在本研究中，我们发现其他K-134结合蛋白的药物-西方的方法。我们分离了两个克隆，可以直接结合K-134，cofilin-2，和CD 36在体外。它们的氨基酸序列的比较显示在CD 36的胶原结合区的一段短的[KxxxxxIxWxxE]上具有相似性。K-134抑制CD 36和I型胶原之间的结合;然而，其他PDE 3抑制剂西洛他唑、氨力农和K-134的无活性衍生物4S-OH-K-134对结合几乎没有影响。结果表明，K-134与CD 36的直接结合是K-134的特征性作用，而同源拉伸可能是K-134与CD 36结合所必需的。这些结果还表明，这些相互作用涉及K-134的抗血小板和抗增生作用的机制。
K-134 ((–)-6-[3-[3-cyclopropyl-3-[(1R, 2R)-2-hydroxycyclohexyl]ureido]-propoxy]-2(1H)-quinolinone) is a novel anti-platelet agent with anti-hyperplastic activities. We found previously that K-134 is a potent phosphodiesterase-3 (PDE3) inhibitor. In the present study, we found other K-134-binding proteins by Drug-Western method. We isolated two clones that can bind directly to K-134, cofilin-2, and CD36 in vitro. Comparison of their amino acid sequences showed similarity over a short stretch [KxxxxVxIxWxxE] in part in the collagen-binding region of CD36. K-134 inhibited binding between CD36 and collagen type-I; however, other PDE3 inhibitors, cilostazol, amrinone, and an inactive derivative of K-134, 4S-OH-K-134, showed little or no effect on binding. It was strongly suggested that the direct binding between K-134 and CD36 is a characteristic effect of K-134, and the homologous stretch may be necessary for binding to K-134. These results also suggested that these interactions are involved in the mechanisms of the anti-platelet and anti-hyperplastic effects of K-134.
影响因子：
20.3
作者：
D. Greenwalt;Robert Lipsky;C. Ockenhouse;H. Ikeda;N. Tandon;G. Jamieson
通讯作者：
D. Greenwalt;Robert Lipsky;C. Ockenhouse;H. Ikeda;N. Tandon;G. Jamieson
CD36 (GPIV) 抗体在流动条件下抑制血小板粘附至内皮下表面。
DOI：
10.1161/01.atv.16.7.883
发表时间：
1996
期刊：
Arteriosclerosis, thrombosis, and vascular biology
影响因子：
--
作者：
Diaz-Ricart,M;Tandon,NN;Gómez-Ortiz,G;Carretero,M;Escolar,G;Ordinas,A;Jamieson,GA
通讯作者：
Jamieson,GA