Department of Physiology & Biophysics, Stony Brook University, Stony Brook, New York, United States of America.
PLoS One. 2012;7(8):e41067. doi: 10.1371/journal.pone.0041067. Epub 2012 Aug 8.
Phospholipase Cβ2 (PLC β2) is activated by G proteins and generates calcium signals in cells. PLCβ2 is absent in normal breast tissue, but is highly expressed in breast tumors where its expression is correlated with the progression and migration of the tumor. This pattern of expression parallels the expression of the breast cancer specific gene protein 1 which is also known as γ-synuclein. The cellular function of γ-synuclein and the role it plays in proliferation are unknown. Here, we determined whether γ-synuclein can interact with PLCβ2 and affect its activity. Using co-immunprecitation and co-immunofluorescence, we find that in both benign and aggressive breast cancer cell lines γ-synuclein and PLCβ2 are associated. In solution, purified γ-synuclein binds to PLCβ2 with high affinity as measured by fluorescence methods. Protease digestion and mass spectrometry studies show that γ-synuclein binds to a site on the C-terminus of PLCβ2 that overlaps with the Gαq binding site. Additionally, γ-synuclein competes for Gαq association, but not for activators that bind to the N-terminus (i.e. Rac1 and Gβγ). Binding of γ-synuclein reduces the catalytic activity of PLCβ2 by mechanism that involves inhibition of product release without affecting membrane interactions. Since activated Gαq binds more strongly to PLCβ2 than γ-synuclein, addition of Gαq(GTPγS) to the γ-synuclein -PLCβ2 complex allows for relief of enzyme inhibition along with concomitant activation. We also find that Gβγ can reverse γ-synuclein inhibition without dissociating the γ-synuclein- PLCβ2- complex. These studies point to a role of γ-synuclein in promoting a more robust G protein activation of PLCβ2.
磷酯酶 Cβ2(PLCβ2)可被 G 蛋白激活,并在细胞中产生钙信号。PLCβ2 在正常乳腺组织中不存在,但在乳腺肿瘤中高度表达,其表达与肿瘤的进展和迁移相关。这种表达模式与乳腺癌特异性基因蛋白 1 的表达模式相似,后者也被称为γ-突触核蛋白。γ-突触核蛋白的细胞功能及其在增殖中的作用尚不清楚。在这里,我们确定了γ-突触核蛋白是否可以与 PLCβ2 相互作用并影响其活性。通过共免疫沉淀和共免疫荧光,我们发现γ-突触核蛋白和 PLCβ2 在良性和侵袭性乳腺癌细胞系中均相关。在溶液中,如荧光法所测,纯化的γ-突触核蛋白与 PLCβ2 具有高亲和力结合。蛋白酶消化和质谱研究表明,γ-突触核蛋白与 PLCβ2 的 C 端结合,该结合位点与 Gαq 结合位点重叠。此外,γ-突触核蛋白竞争与 Gαq 结合,但不与结合到 N 端的激活剂(即 Rac1 和 Gβγ)结合。γ-突触核蛋白的结合通过抑制产物释放而不影响膜相互作用的机制降低 PLCβ2 的催化活性。由于激活的 Gαq 与 PLCβ2 的结合比γ-突触核蛋白更强,因此向γ-突触核蛋白 -PLCβ2 复合物中添加 Gαq(GTPγS)可在同时激活的情况下缓解酶抑制。我们还发现 Gβγ 可以逆转γ-突触核蛋白抑制而不分离γ-突触核蛋白 -PLCβ2- 复合物。这些研究表明γ-突触核蛋白在促进 PLCβ2 更强烈的 G 蛋白激活中起作用。