May 23, 2016 · MYC directly binds to AURKA, and inhibition of this protein–protein interaction by conformation-changing AURKA inhibitors results in subsequent MYC degradation and cell death.

Jan 6, 2009 · AURKA is an oncogene that is amplified in many human tumors, and the encoded kinase Aurora A is a target for current drug development. Here we identify Aurora A as a protein that binds to and stabilizes N-Myc.

In this study, we revealed that AURKA inhibitors exhibited high therapeutic efficacy against RB both in vitro and in vivo. Mechanistically, we found that MYCN could bind to the AURKA promoter region to regulate its transcription, thereby promoting AURKA expression and consequently driving RB progression.

AURKA and MYCN amplifications occur early and are present in hormone naïve tumors from patients who ultimately progress to t-NEPC after androgen deprivation therapy (Figure 5).

Aurora kinase A (encoded by AURKA) is aberrantly expressed in many cancers , including GBM (129–132), making it a plausible candidate for a targeted GBM therapy. Expression of both AURKA and AURKB (Aurora kinase B) is tightly regulated by MYC transcription factor .

We show that, in vitro, the drugs act synergistically to inhibit viability in four models of high-risk neuroblastoma. We demonstrate that this synergy is driven, in part, by the ability of I-BET151 to mitigate reflexive upregulation of AURKA, MYC, and MYCN in response to AURKA inhibition.

AURKA amplification was identified in overall 65% of PCAs (hormone naïve and treated) from patients that developed t-NEPC and in 86% of metastases. Concurrent amplification of MYCN was present in 70% of primary PCAs, 69% of treated PCAs, and 83% of metastases.

We show that cells treated with alisertib have a reflexive transcriptional upregulation of AURKA, MYC, and MYCN, but concomitant treatment with I-BET151 represses that upregulation. Treatment with both drugs is more effective at repressing expression of multiple oncoproteins, including MYC, MYCN, CDK4/6, AURKA, and BCL2.

Sep 1, 2024 · Aurora kinase A (AURKA) is a critical mitotic regulator that stabilizes MYCN by sequestering it from the ubiquitin-proteasome system in MYCN-driven tumors. 14 AURKA belongs to the aurora kinase family of serine/threonine kinases: AURKA, aurora kinase B (AURKB), and aurora kinase C.

Jan 6, 2009 · In a shRNA screen of genes that are highly expressed in MYCN-amplified tumors, we have identified AURKA as a gene that is required for the growth of MYCN-amplified neuroblastoma cells but largely dispensable for cells lacking amplified MYCN.