Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß

Kremer L, Hennes E, Brause A, Ursu A, Robke L, Matsubayashi HT, Nihongaki Y, Flegel J, Mejdrová I, Eickhoff J, Baumann M, Nencka R, Janning P, Kordes S, Schöler HR, Sterneckert J, Inoue T, Ziegler S, Waldmann H (2019). Angew Chem Int Ed Engl

doi: 10.1002/anie.201907632.

The Waldmann lab discoverd the novel Hedgehog (Hh) Pathway inhibitor Pipinib by cell-based screening. Pipinib selectively inhibits phosphatidylinositol 4-kinase IIIβ (PI4KB) and suppresses GLI-mediated transcription and Hh target gene expression by impairing Smoothend (SMO) translocation to the cilium. Thus, PI4KB may be a relevant target protein for inhibition of Hh signaling.  
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