Harlan J E, Hajduk P J, Yoon H S, Fesik S W
Abbott Laboratories, Pharmaceutical Discovery Division, Illinois 60064.
Nature. 1994 Sep 8;371(6493):168-70. doi: 10.1038/371168a0.
The pleckstrin homology (PH) domain is a new protein module of around 100 amino acids found in several proteins involved in signal transduction. Although its specific function has yet to be elucidated, the carboxy-terminal regions of many PH domains bind to the beta gamma subunits of G proteins. On the basis of structural similarities between PH domains and lipid-binding proteins, we have proposed that PH domains may be binding to lipophilic molecules. Indeed, many of the proteins that contain this domain associate with phospholipid membranes, and disruption of this domain can interfere with membrane association. Here we report that PH domains bind to phosphatidylinositol-4,5-bisphosphate and show that the lipid-binding site is located at the lip of the beta-barrel. This suggests that PH domains may be important for membrane localization of proteins through interactions with phosphatidylinositol-4,5-bisphosphate.
普列克底物蛋白同源(PH)结构域是一种新的蛋白质模块,约由100个氨基酸组成,存在于几种参与信号转导的蛋白质中。尽管其具体功能尚待阐明,但许多PH结构域的羧基末端区域可与G蛋白的βγ亚基结合。基于PH结构域与脂质结合蛋白之间的结构相似性,我们推测PH结构域可能与亲脂性分子结合。事实上,许多含有该结构域的蛋白质都与磷脂膜相关,破坏该结构域会干扰膜结合。在此我们报告PH结构域可与磷脂酰肌醇-4,5-二磷酸结合,并表明脂质结合位点位于β桶的边缘。这表明PH结构域可能通过与磷脂酰肌醇-4,5-二磷酸相互作用,对蛋白质的膜定位具有重要作用。