Cozier G E, Lockyer P J, Reynolds J S, Kupzig S, Bottomley J R, Millard T H, Banting G, Cullen P J
Department of Biochemistry, School of Medical Sciences, University of Bristol, Bristol BS8 1TD, United Kingdom.
J Biol Chem. 2000 Sep 8;275(36):28261-8. doi: 10.1074/jbc.M000469200.
The group I family of pleckstrin homology (PH) domains are characterized by their inherent ability to specifically bind phosphatidylinositol 3,4,5-trisphosphate (PtdIns(3,4,5)P(3)) and its corresponding inositol head-group inositol 1,3,4,5-tetrakisphosphate (Ins(1,3,4,5)P(4)). In vivo this interaction results in the regulated plasma membrane recruitment of cytosolic group I PH domain-containing proteins following agonist-stimulated PtdIns(3,4,5)P(3) production. Among group I PH domain-containing proteins, the Ras GTPase-activating protein GAP1(IP4BP) is unique in being constitutively associated with the plasma membrane. Here we show that, although the GAP1(IP4BP) PH domain interacts with PtdIns(3,4, 5)P(3), it also binds, with a comparable affinity, phosphatidylinositol 4,5-bisphosphate (PtdIns(4,5)P(2)) (K(d) values of 0.5 +/- 0.2 and 0.8 +/- 0.5 microm, respectively). Intriguingly, whereas this binding site overlaps with that for Ins(1,3,4,5)P(4), consistent with the constitutive plasma membrane association of GAP1(IP4BP) resulting from its PH domain-binding PtdIns(4,5)P(2), we show that in vivo depletion of PtdIns(4,5)P(2), but not PtdIns(3,4,5)P(3), results in dissociation of GAP1(IP4BP) from this membrane. Thus, the Ins(1,3,4,5)P(4)-binding PH domain from GAP1(IP4BP) defines a novel class of group I PH domains that constitutively targets the protein to the plasma membrane and may allow GAP1(IP4BP) to be regulated in vivo by Ins(1,3,4,5)P(4) rather than PtdIns(3,4,5)P(3).
普列克底物蛋白同源性(PH)结构域的I类家族的特点是具有特异性结合磷脂酰肌醇3,4,5-三磷酸(PtdIns(3,4,5)P(3))及其相应的肌醇头部基团1,3,4,5-四磷酸肌醇(Ins(1,3,4,5)P(4))的内在能力。在体内,这种相互作用导致在激动剂刺激产生PtdIns(3,4,5)P(3)后,含I类PH结构域的胞质蛋白在质膜上的募集受到调控。在含I类PH结构域的蛋白中,Ras GTP酶激活蛋白GAP1(IP4BP)独特之处在于其与质膜组成性结合。在此我们表明,尽管GAP1(IP4BP)的PH结构域与PtdIns(3,4,5)P(3)相互作用,但它也以相当的亲和力结合磷脂酰肌醇4,5-二磷酸(PtdIns(4,5)P(2))(解离常数分别为0.5±0.2和0.8±0.5微摩尔)。有趣的是,虽然这个结合位点与Ins(1,3,4,5)P(4)的结合位点重叠,这与GAP1(IP4BP)因其PH结构域结合PtdIns(4,5)P(2)而与质膜组成性结合一致,但我们表明在体内耗尽PtdIns(4,5)P(2)而非PtdIns(3,4,5)P(3)会导致GAP1(IP4BP)从该膜上解离。因此,GAP1(IP4BP)的Ins(1,3,4,5)P(4)结合PH结构域定义了一类新型的I类PH结构域,其将该蛋白组成性靶向质膜,并可能使GAP1(IP4BP)在体内受Ins(1,3,4,5)P(4)而非PtdIns(3,4,5)P(3)的调控。