https://ogma.newcastle.edu.au/vital/access/ /manager/Index ${session.getAttribute("locale")} 5 Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:51640 Wed 28 Feb 2024 15:44:33 AEDT ]]> Repurposing existing therapeutics, its importance in oncology drug development: Kinases as a potential target https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:45654 Wed 02 Nov 2022 15:37:57 AEDT ]]> Combined In Silico and In Vitro Evidence Supporting an Aurora A Kinase Inhibitory Role of the Anti-Viral Drug Rilpivirine and an Anti-Proliferative Influence on Cancer Cells https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:51615 Tue 12 Sep 2023 13:50:05 AEST ]]> A novel compound which sensitizes BRAF wild-type melanoma cells to vemurafenib in a TRIM16-dependent manner https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:25129 V600E/K mutation. In melanoma cells, loss of TRIM16 expression is a marker of cell migration and metastasis, while the BRAF inhibitor, vemurafenib, induces melanoma cell growth arrest in a TRIM16-dependent manner. Here we identify a novel small molecule compound which sensitized BRAF wild-type melanoma cells to vemurafenib. High throughput, cell-based, chemical library screening identified a compound (C012) which significantly reduced melanoma cell viability, with limited toxicity for normal human fibroblasts. When combined with the BRAFV600E/K inhibitor, vemurafenib, C012 synergistically increased vemurafenib potency in 5 BRAFWT and 4 out of 5 BRAFV600E human melanoma cell lines (Combination Index: CI < 1), and, dramatically reduced colony forming ability. In addition, this drug combination was significantly anti-tumorigenic in vivo in a melanoma xenograft mouse model. The combination of vemurafenib and C012 markedly increased expression of TRIM16 protein, and knockdown of TRIM16 significantly reduced the growth inhibitory effects of the vemurafenib and C012 combination. These findings suggest that the combination of C012 and vemurafenib may have therapeutic potential for the treatment of melanoma, and, that reactivation of TRIM16 may be an effective strategy for patients with this disease.]]> Thu 28 Oct 2021 12:37:19 AEDT ]]>