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Arrest in the G0/G1 phase was associated with downregulation of the transcription factor E2F-1 and its target gene TS.
Constitutive expression of E2F-1 leads to p21-dependent cell cycle arrest in S phase of the cell cycle.
Regulation of FGF receptor-2 expression by transcription factor E2F-1.
The company's lead ACT program, based on the E2F-1 pathway, is partnered with Roche.
Induction of the cellular E2F-1 promoter by, the adenovirus E4-6/7 protein.
that relate to the ongoing development of: ARQ 621, a novel inhibitor of the Eg5 kinesin motor protein in Phase 1 clinical testing; ARQ 736, a novel inhibitor of BRAF in pre-clinical development; and ARQ 501, an activator of the DNA damage response mechanism mediated by the E2F-1 transcription factor that has completed initial clinical testing.
MCF10A (E) and 184A1 (F) cells were treated with BPA (10 nM) for up to 24 hr, and total lysates from these cells were subjected to Western blotting using c-Myc, cyclin D1, cyclin E, E2F-1, and [beta]-actin antibodies.
Similarly, the suppression of Akt-1 in the ERBB-2/Akt signaling pathway can inhibit E2F-1 (a protein with a crucial role in controlling cell cycle progression) and induce [G.
Expression of the cell-cycle-related proteins E2F-1, p53, mdm-2, p21 (waf1), and Ki-67 in multiple myeloma: correlation with cyclin-D1 immunoreactivity.
An additional clinical-stage program includes compounds that activate the cell's DNA damage response mechanism mediated by the E2F-1 transcription factor.
In addition, consistent with the induction of G1/S phase cell population in flow cytometry, downregulation of c-Myc, cyclin D1 D3, CDK4, E2F-1, as well as dephosphorlyation of cdc2 by western blot analysis, as evidenced by the appearance of cell cycle arrest, were observed in Hep3B cells treated with neferine.
E2F-1 is believed to be the ultimate mediator of G1 to S progression by promoting the transcription of a wide range of genes essential for S phase, including cdc25A, cyclin E, and B-myb.
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