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Drug intelligence / Profile preview
Glabrescione B is a naturally occurring methoxyisoflavone, originally isolated from the seeds of *Derris glabrescens*, that acts as a selective, direct inhibitor of the GLI1 transcription factor. GLI1 is a key downstream effector of the Hedgehog (Hh) signaling pathway, which is aberrantly activated in various malignancies. Glabrescione B binds directly to the zinc finger domain of GLI1, disrupting its interaction with DNA and suppressing Hh-mediated transcription. Preclinical studies have demonstrated its efficacy in reducing cell proliferation, self-renewal, and clonogenicity in Hedgehog-dependent cancers, including medulloblastoma, glioma, basal cell carcinoma, and intrahepatic cholangiocarcinoma. To overcome its poor water solubility, researchers have developed advanced delivery systems, such as mPEG5kDa-cholane micelles and hyaluronic acid (HA) nanohydrogels.
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