2018年11月9日 · Here we show that deletion of AF-1 or AF-2 blocks pubertal ductal growth and subsequent development because both are required for expression of essential paracrine mediators. Thirty percent of...

Our data supports this suggestion, with SRC1 bridging AF1 and AF2 by means of interactions between the glutamine-rich region and TAU5 and between the LXXLL motifs and AF2. Clearly, the interaction of SRC1 with AF2 is also important, as evidenced by the inactivating effects of helix 12 mutations and the fact that the M123 mutant in some ...

2023年7月24日 · 生理情况下，雌激素与er结合后，激活er上的转录活性区域af1和af2，促进靶基因转录并最终促进细胞增殖。 ER拮抗药TAM与E2竞争性结合ER，但仅使AF2失活，而AF1活性依然存在，且有类雌激素作用。

EIQPN interacted with the AR-activation fragment-1 (AF-1) domain and blocked its androgen-independent activity, robustly decreased the protein levels of AR and variants in prostate cancer cells by inducing AR protein degradation, and inhibited the androgen-independent proliferation of various AR-positive prostate cancer cells.

2003年10月1日 · Structural Changes in AF-1 by Means Other than Coregulator Binding. Posttranscriptional events such as phosphorylation have been shown to affect the transcriptional activity of certain NRs (e.g. steroid receptors) ().In contrast to AF-2, the AF-1 of these receptors contains many phosphorylation sites, and it may be possible that phosphorylation of AF-1 influences the folding of the AF-1 domain ...

2000年8月8日 · We demonstrate here that TIF2 is able to bind to the isolated AF1 and AF2 simultaneously using distinct interfaces and that this simultaneous interaction can lead to synergistic activation of transcription.

Here we demonstrate that p160 coactivators such as SRC1 (steroid receptor coactivator 1) interact directly with the N terminus in a ligand-independent manner via a conserved glutamine-rich region between residues 1053 and 1123.

2012年12月4日 · We recently showed that two point mutations converting leucines 543 and 544 to alanines in helix 12 (AF2ER) minimized estrogen-dependent AF-2 transcriptional activation. A characteristic feature of AF2ER is that the estrogen antagonists ICI182780 and tamoxifen (TAM) act as agonists through intact AF-1, but not through mutated AF-2.

The steroid receptor coactivator-1 contains multiple receptor interacting and activation domains that cooperatively enhance the activation function 1 (AF1) and AF2 domains of steroid receptors. J. Biol.

We observed AF1-derived AF2 cells, identified by coexpression of Notch3-ICD and Pdgfra-lineage reporter (tdTomato), spatially enriched within the severely damaged regions of the lung that contain dysplastic Krt5 + epithelium .