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Related Concept Videos

Prodrugs01:30

Prodrugs

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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...
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Targeted Cancer Therapies02:57

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Drug Metabolism: Phase II Reactions01:14

Drug Metabolism: Phase II Reactions

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Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
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Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

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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.
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Proton Therapy Delivery and Its Clinical Application in Select Solid Tumor Malignancies
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Proton Therapy Delivery and Its Clinical Application in Select Solid Tumor Malignancies

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Switching on prodrugs using radiotherapy.

Jin Geng1,2, Yichuan Zhang3,4, Quan Gao4

  • 1EaStCHEM School of Chemistry, University of Edinburgh, Edinburgh, UK. jin.geng@siat.ac.cn.

Nature Chemistry
|June 11, 2021
PubMed
Summary
This summary is machine-generated.

This study introduces a novel method for activating cancer prodrugs using gamma/X-ray irradiation. This approach enables localized chemotherapy, reducing systemic toxicity and enhancing targeted cancer treatment.

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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction

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Area of Science:

  • Oncology
  • Radiochemistry
  • Drug Delivery

Background:

  • Systemic toxicity is a major limitation of conventional chemotherapy.
  • Current chemo-radiotherapy strategies often rely on radiosensitization for enhanced efficacy.
  • There is a need for targeted drug delivery to minimize side effects.

Purpose of the Study:

  • To demonstrate a chemistry-based strategy for activating cancer prodrugs using ionizing radiation.
  • To enable simultaneous chemo-radiotherapy with localized prodrug activation.
  • To explore site-directed chemotherapy with real-time drug release at the tumor site.

Main Methods:

  • Utilized gamma/X-ray irradiation to mediate prodrug activation.
  • Showcased activation of a fluorescent probe as a proof of concept.
  • Demonstrated liberation of pazopanib and doxorubicin prodrugs using caged sulfonyl azide and phenyl azide moieties.
  • Employed clinically relevant doses of ionizing radiation.

Main Results:

  • Successfully activated a fluorescent probe via irradiation-mediated chemistry.
  • Liberated active pazopanib and doxorubicin from their caged prodrugs using ionizing radiation.
  • Established proof of concept for localized, radiation-activated chemotherapy.

Conclusions:

  • Developed a novel strategy for radiation-mediated, site-directed prodrug activation.
  • This approach offers a new paradigm for targeted chemotherapy, distinct from conventional chemo-radiotherapy.
  • Potential to revolutionize cancer treatment by enabling localized drug release at the tumor site.