Alevizopoulos K, Sanchez B, Amati B
Swiss Institute for Experimental Cancer Research, Epalinges.
Oncogene. 2000 Apr 13;19(16):2067-74. doi: 10.1038/sj.onc.1203534.
Ectopic expression of the CDK inhibitors (CKIs) p16INK4a and p27Kip1 in Rat1 fibroblasts induces dephosphorylation and activation of Retinoblastoma-family proteins (pRb, p107 and p130), their association with E2F proteins, and cell cycle arrest in G1. The growth-inhibitory action of p16, in particular, is believed to be mediated essentially via pRb activation. The 12S E1A protein of human Adenovirus 5 associates with pRb-family proteins via residues in its Conserved Regions (CR) 1 and 2, in particular through the motif LXCXE in CR2. These interactions are required for E1A to prevent G1 arrest upon co-expression of CKIs. We show here that mutating either of two conserved motifs adjacent to LXCXE in CR2, GFP and SDDEDEE, also impairs the ability of E1A to overcome G1 arrest by p16 or p27. Strikingly, however, these mutations affect neither the association of E1A with pRb, p07 and p130, nor its ability to derepress E2F-1 transcriptional activity in transient transfection assays. One of the EIA mutants, however, is defective in derepressing several endogenous E2F target genes in the presence of p16 or p27. Thus, CR2 possesses an essential function besides pRb-binding. We speculate that this function might be required for the full derepression of E2F-regulated genes in their natural chromatin context.
细胞周期蛋白依赖性激酶抑制剂(CKIs)p16INK4a和p27Kip1在大鼠1型成纤维细胞中的异位表达可诱导视网膜母细胞瘤家族蛋白(pRb、p107和p130)去磷酸化并激活,使其与E2F蛋白结合,并导致细胞周期在G1期停滞。特别是,p16的生长抑制作用被认为主要是通过pRb激活介导的。人腺病毒5的12S E1A蛋白通过其保守区域(CR)1和2中的残基与pRb家族蛋白结合,特别是通过CR2中的LXCXE基序。这些相互作用是E1A在与CKIs共表达时防止G1期停滞所必需的。我们在此表明,突变CR2中与LXCXE相邻的两个保守基序之一,即GFP和SDDEDEE,也会损害E1A克服p16或p27诱导的G1期停滞的能力。然而,令人惊讶的是,这些突变既不影响E1A与pRb、p07和p130的结合,也不影响其在瞬时转染实验中解除E2F-1转录活性抑制的能力。然而,其中一个EIA突变体在存在p16或p27的情况下,在解除几个内源性E2F靶基因的抑制方面存在缺陷。因此,CR2除了与pRb结合外还具有重要功能。我们推测,在天然染色质环境中,E2F调控基因的完全去抑制可能需要这一功能。