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Prodrugs01:30

Prodrugs

Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...

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Updated: Jul 4, 2026

Photodynamic Therapy with Blended Conducting Polymer/Fullerene Nanoparticle Photosensitizers
09:45

Photodynamic Therapy with Blended Conducting Polymer/Fullerene Nanoparticle Photosensitizers

Published on: October 28, 2015

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Green Light Activated Dual-Action Pt(IV) Prodrug with Enhanced PDT Activity.

Daniil Spector1, Vladislav Bykusov1, Yulia Isaeva2,3

  • 1Chemistry Department, Lomonosov Moscow State University, Leninskie gory 1,3, 119991, Moscow, Russia.

Chemmedchem
|January 10, 2025
PubMed
Summary

Green light activates a novel platinum(IV) prodrug, GreenPt, for precise cancer therapy. This dual-action drug releases cisplatin and a photosensitizer, enhancing treatment efficacy with minimal light dose.

Keywords:
BODIPYPDTProdrugcisplatinphotoactivation

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Area of Science:

  • Biochemistry
  • Materials Science
  • Oncology

Background:

  • Platinum(IV) prodrugs offer spatiotemporal control over chemotherapy.
  • Combining chemotherapy with photodynamic therapy (PDT) can overcome limitations of individual treatments.

Purpose of the Study:

  • To develop a green-light-activated Pt(IV) prodrug (GreenPt) combining chemotherapy and PDT.
  • To investigate the mechanism of light-induced cisplatin release and evaluate its phototoxicity.

Main Methods:

  • Synthesis and characterization of GreenPt prodrug.
  • Green light irradiation studies for cisplatin release.
  • Density Functional Theory (DFT) modeling and photoinduced electron transfer (PET) estimation.
  • In vitro phototoxicity assays.

Main Results:

  • GreenPt releases cisplatin under low-dose green light (1 J/cm²).
  • DFT and PET analysis identified photoinduced electron transfer as the key release mechanism.
  • BODIPY-based photosensitizers exhibited high phototoxicity (PI > 1300).
  • GreenPt showed light-induced phototoxicity (PI > 100) and intracellular accumulation.

Conclusions:

  • GreenPt is a highly efficient green-light-activated prodrug for dual-action cancer therapy.
  • The study elucidates the mechanism of light-induced cisplatin release from Pt(IV) prodrugs.
  • GreenPt demonstrates potential for synergistic therapeutic effects via controlled release of cisplatin and a photosensitizer.