Related Experiment Video

Updated: Sep 29, 2025

RhoC GTPase Activation Assay
09:58

RhoC GTPase Activation Assay

Published on: August 22, 2010

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Knockdown of RhoA Expression Reverts Enzalutamide Resistance via the p38 MAPK Pathway in Castration-resistant

Xiaoliang Chen1, Lili Yin2, Hui Xu3

  • 1Schools of Medicine, Datong University, Datong, Shanxi, 037009, P.R. China.

Recent Patents on Anti-Cancer Drug Discovery
|March 27, 2022
PubMed
Abstract

Insights

RhoA (RHOA) is upregulated in enzalutamide-resistant prostate cancer (PCa). Inhibiting RHOA can overcome resistance and enhance enzalutamide treatment effectiveness in castration-resistant prostate cancer (CRPC).

Area of Science:

  • Oncology
  • Molecular Biology
  • Cancer Research

Background:

  • Enzalutamide is approved for castration-resistant prostate cancer (CRPC) but resistance limits its efficacy.
  • RhoA plays a role in cancer progression, but its function in enzalutamide-resistant prostate cancer (PCa) is not well understood.

Purpose of the Study:

  • To investigate the role of RhoA in enzalutamide resistance in CRPC.
  • To elucidate the mechanisms underlying RhoA depletion's effect on enzalutamide resistance.

Main Methods:

  • Western blotting to assess protein expression (RhoA, ROCK2, p38, AR).
  • MTT and colony formation assays for cell survival and proliferation.
  • Xenograft experiments and H&E staining for in vivo validation.

Main Results:

  • RhoA, ROCK2, p38, and AR expression increased in enzalutamide-resistant PCa cells.
  • Silencing RhoA or ROCK2 reduced proliferation and colony formation in resistant cells.
  • RhoA deletion enhanced enzalutamide efficacy in xenograft models, acting via the RhoA/ROCK2/p38 pathway.

Conclusions:

  • RhoA is a potential therapeutic target for overcoming enzalutamide resistance in CRPC.
  • Inhibiting RhoA can restore sensitivity to enzalutamide, improving treatment outcomes.
Keywords:
CRPCEnzalutamide resistanceRhoAp38 MAPK pathwayprostate cancerxenograft experiments

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