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Urate transporter inhibitor lesinurad is a selective peroxisome proliferator-activated receptor gamma modulator (sPPARγM) in vitro

: Heitel, P.; Gellrich, L.; Heering, J.; Goebel, T.; Kahnt, A.; Proschak, E.; Schubert-Zsilavecz, M.; Merk, D.

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Scientific Reports 8 (2018), Art. 1355, 11 pp.
ISSN: 2045-2322
Journal Article, Electronic Publication
Fraunhofer IME ()

Gout is the most common arthritic disease in human but was long neglected and therapeutic options are not satisfying. However, with the recent approval of the urate transporter inhibitor lesinurad, gout treatment has experienced a major innovation. Here we show that lesinurad possesses considerable modulatory potency on peroxisome proliferator-activated receptor γ (PPARγ). Since gout has a strong association with metabolic diseases such as type 2 diabetes, this side-activity appears as very valuable contributing factor to the clinical efficacy profile of lesinurad. Importantly, despite robustly activating PPARγ in vitro, lesinurad lacked adipogenic activity, which seems due to differential coactivator recruitment and is characterized as selective PPARγ modulator (sPPARγM).