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Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer

Joseph M Salvino1, Yellamelli V V Srikanth1, Rongliang Lou2

  • 1Department of Pharmacology and Physiology, Drexel University College of Medicine, 245 N 15th Street, Philadelphia, PA 19102-1101, USA.

Bioorganic & Medicinal Chemistry Letters
|April 8, 2017
PubMed

Insights

Researchers are developing new prostate cancer treatments targeting the Sigma1 protein, which stabilizes the androgen receptor (AR). This approach aims to overcome resistance to current therapies for disseminated and castration-resistant prostate cancer.

Area of Science:

  • Oncology
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • Prostate cancer is a leading cause of cancer death in men.
  • Current treatments for disseminated prostate cancer rely on androgen deprivation therapy (ADT).
  • Tumors frequently develop resistance to ADT, leading to castration-resistant prostate cancer (CRPC).

Purpose of the Study:

  • To investigate novel therapeutic strategies for advanced prostate cancer.
  • To target the Sigma1 protein, a key stabilizer of the androgen receptor (AR).
  • To develop new Sigma1-targeting compounds for lead optimization to overcome treatment resistance.

Main Methods:

  • Utilizing a hybrid pharmacophore approach to design new compounds.
  • Focusing on Sigma1 (sigma-1 receptor), a 26-kDa integral membrane protein.
  • Lead optimization of novel Sigma1-targeting agents.

Main Results:

  • A new series of Sigma1 compounds has been synthesized.
  • These compounds are derived from a hybrid pharmacophore strategy.
  • The study reports on the lead optimization of these novel agents.

Conclusions:

  • Targeting Sigma1 represents a promising strategy for overcoming resistance in prostate cancer.
  • The developed Sigma1 compounds offer potential for more effective treatments.
  • This research contributes to the development of next-generation therapies for advanced prostate cancer.
Keywords:
GuanidineProstate cancerSigma-1 chaperoneSigma-1 receptorSigma1Small molecule inhibitor

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