Publications by authors named "Laura S Collins"
Article Synopsis
- Enzymatic inhibition of histone deacetylase (HDAC) is a promising strategy for cancer treatment, leading to the development of new amide derivatives.
- Several of these compounds demonstrated strong HDAC inhibitory effects, with low IC(50) values in nanomolar ranges when tested on HeLa cells.
- The novel compounds, particularly one called (E)-N-[6-(hydroxyamino)-6-oxohexyl]-3-(7-quinolinyl)-2-propenamide, showed impressive results in vivo, significantly increasing the lifespan of mice with leukemia.
The human HDAC (histone deacetylase) family, a well-validated anticancer target, plays a key role in the control of gene expression through regulation of transcription. While HDACs can be subdivided into three main classes, the class I, class II and class III HDACs (sirtuins), it is presently unclear whether inhibiting multiple HDACs using pan-HDAC inhibitors, or targeting specific isoforms that show aberrant levels in tumours, will prove more effective as an anticancer strategy in the clinic. To address the above issues, we have tested a number of clinically relevant HDACis (HDAC inhibitors) against a panel of rhHDAC (recombinant human HDAC) isoforms.
View Article and Find Full Text PDFPurpose: Histone deacetylase inhibitors (HDACi) inhibit the growth of cancer cells, and combinations of HDACi with established chemotherapeutics can lead to synergistic effects. We have investigated effects of PXD101 (HDACi in phase II clinical trials) in combination with 5-fluorouracil, on tumour cell proliferation and apoptosis both in vitro and in vivo.
Experimental Design: HCT116 cells were studied using proliferation and clonogenic assays.