The G-protein-coupled estrogen receptor agonist G-1 suppresses proliferation of ovarian cancer cells by blocking tubulin polymerization.
The G-protein-coupled estrogen receptor agonist G-1 suppresses proliferation of ovarian cancer cells by blocking tubulin polymerization.
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DOI：
10.1038/cddis.2013.397
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发表时间：
2013-10-17
影响因子：
9
通讯作者：
中科院分区：
文献类型：
--
作者：
g蛋白偶联雌激素受体1 （GPER）最近被报道在不同类型的细胞和组织中介导雌激素的非基因组作用。G-1（1-[4-（6-溴苯并[1,3]二恶醇-5基）-3a,4,5,9b-四氢- 3h -环五[c]喹啉-8基]-乙酮）是一种有效的选择性GPER激动剂。G-1已被证明可以通过激活GPER来诱导基因的表达并激活促进癌细胞增殖的途径。在这里，我们证明了G-1具有抗癌潜力，其机制类似于常用的化疗药物长春花生物碱。我们发现G-1阻断微管蛋白聚合，从而中断卵巢癌细胞中的微管组装，导致有丝分裂前期细胞周期停滞，抑制卵巢癌细胞增殖。G-1也可诱导卵巢癌细胞凋亡。G-1靶向微管抑制卵巢癌细胞增殖的能力使其成为治疗卵巢癌的有希望的候选药物。
The G-protein-coupled estrogen receptor 1 (GPER) has recently been reported to mediate the non-genomic action of estrogen in different types of cells and tissues. G-1 (1-[4-(6-bromobenzo[1,3] dioxol-5yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone) was developed as a potent and selective agonist for GPER. G-1 has been shown to induce the expression of genes and activate pathways that facilitate cancer cell proliferation by activating GPER. Here we demonstrate that G-1 has an anticancer potential with a mechanism similar to vinca alkaloids, the commonly used chemotherapy drugs. We found that G-1 blocks tubulin polymerization and thereby interrupts microtubule assembly in ovarian cancer cells leading to the arrest of cell cycle in the prophase of mitosis and the suppression of ovarian cancer cell proliferation. G-1 treatment also induces apoptosis of ovarian cancer cells. The ability of G-1 to target microtubules to suppress ovarian cancer cell proliferation makes it a promising candidate drug for treatment of ovarian cancer.
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影响因子：
12.4
作者：
通讯作者：
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影响因子：
11.2
作者：
Ariazi EA;Brailoiu E;Yerrum S;Shupp HA;Slifker MJ;Cunliffe HE;Black MA;Donato AL;Arterburn JB;Oprea TI;Prossnitz ER;Dun NJ;Jordan VC
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DOI：
10.1016/j.bbrc.2012.02.161
发表时间：
2012-04-06
影响因子：
3.1
作者：
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通讯作者：
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影响因子：
5.7
作者：
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通讯作者：
Wan, Xiao-Ping
影响因子：
3.7
作者：
Chevalier N;Vega A;Bouskine A;Siddeek B;Michiels JF;Chevallier D;Fénichel P
通讯作者：
Fénichel P