Thioredoxin-interacting protein (TXNIP) has emerged as an important regulator of key cellular processes including metabolic disorders, cancer and inflammation. Type 2 diabetes mellitus (T2DM) is characterized by a defect in insulin secretion and action and recent studies showed that TXNIP is implicated in pancreatic β-cell glucose toxicity. Moreover, it has been shown that TxNIP is among the most highly regulated gene in β-cells exposed to high glucose glucose. In this context, TXNIP has emerged as an attractive target for T2DM and for the promotion of endogenous β-cell mass and insulin production. In this poster, we describe the discovery and optimization of orally available small molecule probes that would allow further exploration of the role of TXNIP in T2DM prevention but also reversion.

Optimized chemical tools to probe the function of thioredoxin-interacting protein as therapeutic target

253rd National Meeting (2017)

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