Nobuhisa I, Chiwata T, Fukumaki Y, Hattori S, Shimohigashi Y, Ohno M
Department of Chemistry, Faculty of Science, Kyushu University, Fukuoka, Japan.
FEBS Lett. 1998 Jun 16;429(3):385-9. doi: 10.1016/s0014-5793(98)00602-4.
Five inhibitors (PLI-I-V) against Trimeresurus flavoviridis (Tf, habu snake, Crotalinae) venom phospholipase A2 (PLA2) isozymes have been isolated from its serum. PLI-I, which is composed of two repeated three-finger motifs, and PLI-IV and PLI-V, which contain a sequence similar to the carbohydrate recognition domain (CRD) of C-type lectins, were expressed in the forms fused with glutathione S-transferase (GST). The resulting GST-PLIs showed ability to bind to three Tf venom PLA2 isozymes. The binding study with the truncated forms indicated that one of two three-finger motifs of PLI-I was able to bind to PLA2 isozymes. The N-terminal 37-amino acid fragment and the CRD-like domain of PLI-IV and PLI-V were bound to PLA2 isozymes. On the other hand, their C-terminal 12-amino acid segment also associated with PLA2 isozymes. When either of two units of a hydrophobic tripeptide in this sequence was replaced by trialanine, the binding was completely abolished, indicating that the C-terminal hydrophobic cores of PLI-IV and PLI-V were critically responsible for the binding to venom PLA2 isozymes.
已从血清中分离出五种针对竹叶青蛇(Tf,蝮蛇,蝰蛇科)毒液磷脂酶A2(PLA2)同工酶的抑制剂(PLI-I-V)。由两个重复的三指基序组成的PLI-I,以及包含与C型凝集素的碳水化合物识别结构域(CRD)相似序列的PLI-IV和PLI-V,以与谷胱甘肽S-转移酶(GST)融合的形式表达。所得的GST-PLIs显示出与三种竹叶青蛇毒液PLA2同工酶结合的能力。对截短形式的结合研究表明,PLI-I的两个三指基序之一能够与PLA2同工酶结合。PLI-IV和PLI-V的N端37个氨基酸片段以及CRD样结构域与PLA2同工酶结合。另一方面,它们的C端12个氨基酸片段也与PLA2同工酶相关。当该序列中疏水性三肽的两个单元中的任何一个被三丙氨酸取代时,结合完全被消除,这表明PLI-IV和PLI-V的C端疏水核心对于与毒液PLA2同工酶的结合至关重要。