DOI: 10.1021/acsmedchemlett.6c00533 ISSN: 1948-5875

Direct STAT6 Inhibition: Benzimidazoles Move Type 2 Inflammation Downstream

Anna C. Renner, Robert B. Kargbo

Abstract

STAT6 translates interleukin-4 and interleukin-13 signaling into type 2 inflammatory programs underlying allergic disease. Belharra Therapeutics discloses substituted benzimidazoles that directly inhibit STAT6, including compounds with submicromolar biochemical activity. The chemistry illustrates growing efforts to intervene downstream of cytokine receptors, potentially offering oral, pathway-focused control of diseases currently dominated by biologics targeting extracellular IL-4/IL-13 signaling.

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