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Natural product-drug conjugates for modulation of TRPV1-expressing tumors

Charlotte Baker1, Tiago Rodrigues1, Bernardo P de Almeida1

  • 1Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Av. Prof. Egas Moniz, 1649-028 Lisboa, Portugal.

Bioorganic & Medicinal Chemistry
|March 20, 2019
PubMed

Insights

Researchers developed novel drug conjugates targeting prostate cancer by leveraging the transient receptor potential vanilloid 1 (TRPV1) channel. A serendipitous discovery suggests a new approach for personalized prostate cancer medicine.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Pharmacology

Background:

  • Prostate cancer often over-expresses the transient receptor potential vanilloid 1 (TRPV1) channel.
  • TRPV1 is a potential therapeutic target for prostate cancer treatment.
  • Targeted drug delivery strategies are needed to improve treatment efficacy.

Purpose of the Study:

  • To design, synthesize, and evaluate natural product-drug conjugates for prostate cancer treatment.
  • To validate TRPV1 as a therapeutic target in prostate cancer.
  • To demonstrate the feasibility of a bioorthogonal drug delivery system.

Main Methods:

  • Bioinformatics analysis to assess TRPV1 relevance in prostate cancer.
  • Synthesis of natural product-drug conjugates.
  • Bioorthogonal chemistry and stability assays.
  • Cell-based assays to evaluate conjugate activity.

Main Results:

  • TRPV1 relevance as a target was validated in prostate cancer patients.
  • The drug delivery strategy was proven feasible under physiological conditions.
  • Synthesized conjugates showed modest activity in cell-based assays.
  • A combination of TRPV1 agonist and cytotoxic agent showed potential.

Conclusions:

  • Natural product-drug conjugates targeting TRPV1 are a viable strategy for prostate cancer.
  • Bioorthogonal chemistry enables effective drug delivery for cancer therapy.
  • A novel combination therapy approach may offer new avenues for personalized prostate cancer medicine.
Keywords:
CancerChemical biologyDrug deliveryLigand-gated ion channelSmall molecule–drug conjugates

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