BRCA1与雌激素受体相互作用的结构决定因素。
Structural determinants of the BRCA1 : estrogen receptor interaction.
作者信息
Ma Yong Xian, Tomita York, Fan Saijun, Wu Kongming, Tong Youzhi, Zhao Zeguo, Song Liang-Nian, Goldberg Itzhak D, Rosen Eliot M
机构信息
Department of Oncology, Lombardi Cancer Center, Georgetown University, 3970 Reservoir Road, NW, Washington, DC 20057, USA.
出版信息
Oncogene. 2005 Mar 10;24(11):1831-46. doi: 10.1038/sj.onc.1208190.
Previously, we showed that the BRCA1 protein interacts directly and functionally with estrogen receptor-alpha (ER-alpha), resulting in the inhibition of estradiol (E2)-stimulated ER-alpha transcriptional activity. The interaction sites were mapped to the N-terminus of BRCA1 (within amino acids (aa) 1-302) and the ligand-binding domain/activation function-2 (LBD/AF-2) region (within aa 282-420) of ER-alpha. In this study, we have further characterized the structure/function relationship for the BRCA1 : ER-alpha interaction. We found that the N-terminal RING domain (aa 20-64) is not required for the BRCA1 : ER-alpha interaction. We identified two separate contact points for ER-alpha, one within aa 1-100 and the other within aa 100-200 of BRCA1; and we showed that each of these BRCA1 peptides interacts with BRCA1 in vitro and in vivo. By using different fragments of the BRCA1 N-terminus, we found that aa 67-100 and 101-133 are required for the interaction with ER-alpha, but that aa 1-67 and 134-302 are dispensible. Previously, we showed that BRCA1 aa 1-302 does not inhibit E2-stimulated ER-alpha transcriptional activity but does bind to ER-alpha and acts as a dominant negative inhibitor of the full-length BRCA1 protein. Somewhat surprisingly, we found that BRCA1 aa 1-100 and BRCA1 aa 101-200 (but not aa 201-300) each inhibited ER-alpha activity, although not as efficiently as full-length BRCA1. Mutations within an HIV Rev-like nuclear export signal that resembles a nuclear receptor corepressor motif (aa 86-95) impaired the ability of both truncated (aa 1-100) and full-length (aa 1-1863) BRCA1 proteins to interact with and/or repress ER-alpha activity. Based on these findings, a partial BRCA1 : ER-alpha three-dimensional structure is proposed. The implications of these findings for understanding the BRCA1 : ER-alpha interaction are discussed.
此前,我们发现BRCA1蛋白与雌激素受体α(ER-α)直接发生功能性相互作用,从而抑制雌二醇(E2)刺激的ER-α转录活性。相互作用位点定位于BRCA1的N端(氨基酸(aa)1 - 302内)以及ER-α的配体结合域/激活功能2(LBD/AF-2)区域(aa 282 - 420内)。在本研究中,我们进一步阐述了BRCA1与ER-α相互作用的结构/功能关系。我们发现BRCA1与ER-α相互作用不需要N端的RING结构域(aa 20 - 64)。我们确定了ER-α的两个独立接触点,一个在BRCA1的aa 1 - 100内,另一个在aa 100 - 200内;并且我们证明这些BRCA1肽段在体外和体内均能与BRCA1相互作用。通过使用BRCA1 N端的不同片段,我们发现aa 67 - 100和101 - 133是与ER-α相互作用所必需的,但aa 1 - 67和134 - 302是不必要的。此前,我们发现BRCA1 aa 1 - 302不抑制E2刺激的ER-α转录活性,但能与ER-α结合并作为全长BRCA1蛋白的显性负性抑制剂。有点令人惊讶的是,我们发现BRCA1 aa 1 - 100和BRCA1 aa 101 - 200(但不是aa 201 - 300)均能抑制ER-α活性,尽管不如全长BRCA1有效。类似于核受体共抑制基序的HIV Rev样核输出信号内的突变(aa 86 - 95)损害了截短型(aa 1 - 100)和全长型(aa 1 - 1863)BRCA1蛋白与ER-α相互作用和/或抑制其活性的能力。基于这些发现,提出了BRCA1与ER-α的部分三维结构。讨论了这些发现对于理解BRCA1与ER-α相互作用的意义。