Drug intelligence / Profile preview

diptoindonesin G

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Diptoindonesin G is a natural resveratrol dimer, a type of stilbenoid, originally isolated from plants such as those in the *Hopea* genus. It is being investigated as a potential therapeutic agent for prostate cancer, including castration-resistant (CRPC) and enzalutamide-resistant forms. The compound's primary mechanism of action involves promoting the proteasomal degradation of the androgen receptor (AR) and polo-like kinase 1 (PLK1). This degradation is mediated through the modulation and activation of the C-terminus of HSC70-interacting protein (CHIP), also known as STUB1, which is an E3 ubiquitin ligase. By reducing the protein levels of these key oncogenic drivers, Diptoindonesin G inhibits cell viability and tumor growth. Preclinical studies have demonstrated that it can also enhance the efficacy of HSP90 inhibitors and enzalutamide in human prostate cancer models.

02

Targets

HSP90 (Heat shock protein 90 chaperone complex)

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