Selective ARTD8 inhibitors to better the understanding of metastatic cancers

A protein known as ARTD8 has been shown to be over expressed in most cancer types and supports the metastases of cancer cells through enhancing tumour growth, accelerating the metabolism and promoting cell survival. Inhibition of ARTD8 has been shown to inhibit DNA repair mechanisms and selectively decrease the metabolism of tumour cells while not effecting the growth of normal non-cancerous cells. This makes ARTD8 an interesting target for selectively targeting metastatic cancers as these once-resistant cancers would be more susceptible to regular anti-cancer therapies.

Currently there is no selective ARTD8 inhibitors and the understanding of how ARTD8 functions has only been studied using knockdown models. To further our understanding of metastatic cancers and work towards developing a treatment more research is needed. Our research team aims to generate a selective inhibitor for ARTD8 to help develop the understanding of metastatic cancers. Work by our team used a de novo computational modelling method followed by organic synthesis of potential inhibitors. The ARTD8 inhibitors, once synthesised and structurally elucidated, were then analysed in chemiluminescence inhibition assays against both ARTD8 and ARTD1 to determine selectivity.