Periodic Reporting for period 1 - RGD-Diabetes (Development of RGD-therapeutics for cardio-metabolic disease)
Okres sprawozdawczy: 2019-12-01 do 2021-11-30
In the current project, RGD-Diabetes, we designed and tested small drug-like molecules with the intention that we could mimic the action of the RGD=sequence and increase the action of insulin on muscle cells. We used computer-based screening approaches to identify 30 compounds which we anticipated would bind to integrin receptors and mimic the actions of the RGD-sequence of IGFBP1. We confirmed that candidate compounds were able to augment insulin-signalling and glucose uptake in cultured skeletal muscle cells and from these successfully identified compounds for further development based on their solubility, stability and other properties. We therefore achieved our project aim, by achieving proof-of-concept that small-molecule mimetics of the RGD-motif of IGFBP1 can enhance insulin action and show promise for drug-development. We now intend to progress this research further towards the development of new therapeutics for diabetes. If successful, development of a new drug to prevent and treat diabetes which also has favourable cardiovascular effects could ultimately help millions of people worldwide.