O'Connell J C, McCallum J F, McPhee I, Wakefield J, Houslay E S, Wishart W, Bolger G, Frame M, Houslay M D
Division of Biochemistry and Molecular Biology, I.B.L.S., University of Glasgow, Scotland, U.K.
Biochem J. 1996 Aug 15;318 ( Pt 1)(Pt 1):255-61. doi: 10.1042/bj3180255.
The PDE4A (type IV) cAMP-specific, rolipram-inhibited phosphodiesterase RPDE-6 (RNPDE4A5), when transiently expressed in COS7 cells, could be complexed with the v-Src-SH3 domain expressed as a glutathione S-transferase (GST) fusion protein. RPDE-6 did not interact with GST itself. This complex was not disrupted by treatment with high NaCl concentration together with Triton X-100. Interaction was apparently determined by the N-terminal splice region of RPDE-6, as the PDE4A splice variant RPDE-39, which differs from RPDE-6 at the extreme N-terminus, failed to associate with v-Src-SH3; met26RD1 (where RD1 is rat 'dunc-like' PDE), which has the N-terminal splice region deleted, failed to associate with v-Src-SH3, and the association of RPDE-6 and v-Src-SH3 was blocked by a fusion protein formed from the N-terminal splice region. RDPE-6 showed binding to GST fusion proteins of both the intact Src kinase and an SH2-SH3 construct but did not bind to the Src-SH2 domain or to the adaptor protein Grb-2. RPDE-6 could be co-immunoprecipitated from cytosol extracts of transfected cells by using anti-Src antiserum. RPDE-6 exhibited selectivity in binding to the SH3 domains of c-Abl, Crk, Csk, Lck, Lyn, Fyn and v-Src, with binding to the SH3 regions of the Src-related tyrosyl kinases Lyn and Fyn being the most effective. The binding of RPDE-6 to the SH3 domains of Crk, Csk and Lck led to a marked reduction in PDE activity, but no change was apparent in complexes with other species. Endogenous RPDE-6 from brain, but not endogenous RPDE-39 from testis, bound to the Src-SH3 domain. We suggest that the PDE4A splice variant RPDE-6 has a propensity for interaction with selective SH3 domains, in particular those from Src and the Src-related tyrosyl kinases Lyn and Fyn. This interaction seems to be governed by alternative splicing of the PDE4A gene, because RPDE-39, a splice variant that lacks the proline-rich N-terminal splice region of RPDE-6, does not interact with these SH3 domains. It is proposed that the binding site on RPDE-6 for SH3 domains lies within the unique first 102 residues of its N-terminal splice domain, where two motifs representing Class I SH3 binding sites with selectivity for Src kinase SH3 domains can be identified and one motif for a putative Class II SH3 binding site.
磷酸二酯酶4A(IV型)特异性作用于环磷酸腺苷(cAMP)、受咯利普兰抑制的磷酸二酯酶RPDE-6(RNPDE4A5),当在COS7细胞中瞬时表达时,可与作为谷胱甘肽S-转移酶(GST)融合蛋白表达的v-Src-SH3结构域形成复合物。RPDE-6不与GST本身相互作用。用高浓度氯化钠和曲拉通X-100处理不会破坏这种复合物。相互作用显然由RPDE-6的N端剪接区域决定,因为在极端N端与RPDE-6不同的磷酸二酯酶4A剪接变体RPDE-39不能与v-Src-SH3结合;met26RD1(其中RD1是大鼠“dunc样”磷酸二酯酶)的N端剪接区域被删除,不能与v-Src-SH3结合,并且RPDE-6与v-Src-SH3的结合被由N端剪接区域形成的融合蛋白阻断。RDPE-6与完整Src激酶和SH2-SH3构建体的GST融合蛋白均显示结合,但不与Src-SH2结构域或衔接蛋白Grb-2结合。使用抗Src抗血清可从转染细胞的胞质提取物中共免疫沉淀出RPDE-6。RPDE-6在与c-Abl、Crk、Csk、Lck、Lyn、Fyn和v-Src的SH3结构域结合方面具有选择性,其中与Src相关的酪氨酸激酶Lyn和Fyn的SH3区域结合最为有效。RPDE-6与Crk、Csk和Lck的SH3结构域结合导致磷酸二酯酶活性显著降低,但与其他种类形成的复合物中未观察到明显变化。来自脑的内源性RPDE-6可与Src-SH3结构域结合,而来自睾丸的内源性RPDE-39则不能。我们认为磷酸二酯酶4A剪接变体RPDE-6倾向于与选择性SH3结构域相互作用,特别是来自Src以及Src相关酪氨酸激酶Lyn和Fyn的SH3结构域。这种相互作用似乎受磷酸二酯酶4A基因的可变剪接调控,因为缺乏RPDE-6富含脯氨酸的N端剪接区域的剪接变体RPDE-39不与这些SH3结构域相互作用。有人提出,RPDE-6上SH3结构域的结合位点位于其N端剪接结构域独特的前102个残基内,在该区域可识别出两个对Src激酶SH3结构域具有选择性的I类SH3结合位点基序以及一个推定的II类SH3结合位点基序。