Drug intelligence / Profile preview

glabrescione B

Development stage
Preclinical
Lead developer
Sapienza University of Rome
Modality
Small Molecules
Administration
Intranasal, Intravenous
01

Overview

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.

Other names
3-[3,4-bis(3-methylbut-2-enoxy)phenyl]-5,7-dimethoxychromen-4-one5,7-dimethoxy-3',4'-diprenyloxyisoflavoneGlaB
02

Targets

GLI1

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