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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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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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Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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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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Combination Therapies and Personalized Medicine02:50

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Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
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Binding sites linkages can regulate a protein's function.  For example, enzyme activity is often regulated through a feedback mechanism where the end product of the biochemical process serves as an inhibitor.
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Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
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Enhancement of Apoptotic and Autophagic Induction by a Novel Synthetic C-1 Analogue of 7-deoxypancratistatin in Human Breast Adenocarcinoma and Neuroblastoma Cells with Tamoxifen
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Pt(IV) Prodrug as a Potential Antitumor Agent with APE1 Inhibitory Activity.

Yi Yuan1, Dingqiang Fu1, Yan Xu1

  • 1Natural Products Research Center, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China.

Journal of Medicinal Chemistry
|November 16, 2022
PubMed
Summary

A new platinum(IV) prodrug, AP1, effectively targets the base excision repair (BER) pathway protein APE1. AP1 shows superior efficacy against resistant cancers and inhibits tumor growth with minimal toxicity.

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Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
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Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The base excision repair (BER) pathway is crucial for cancer cells to develop resistance to chemotherapy.
  • Targeting BER offers a potential strategy to overcome treatment resistance.
  • Apurinic/apyrimidinic endonuclease 1 (APE1) is a key enzyme in the BER pathway.

Purpose of the Study:

  • To develop and evaluate a novel platinum(IV) prodrug, AP1, designed to target APE1.
  • To investigate the mechanism of action and efficacy of AP1 in cancer treatment.
  • To assess the potential of AP1 in overcoming cisplatin resistance.

Main Methods:

  • Synthesis and characterization of the Pt(IV) prodrug AP1.
  • In vitro studies assessing AP1's cytotoxicity against various cancer cell lines, including cisplatin-resistant ones.
  • In vivo efficacy studies using a xenograft cancer model.
  • Investigation of AP1's effect on DNA damage response, apoptosis, and APE1 activity.

Main Results:

  • AP1 demonstrated significant inhibition of cancer cell growth, outperforming cisplatin, especially in resistant cell lines (up to 18.11-fold inhibition).
  • AP1 showed comparable toxicity to normal cells as cisplatin.
  • In vivo studies revealed AP1 to be 3.86-fold more potent than cisplatin without adverse effects.
  • AP1 directly inhibited APE1 endonuclease activity, leading to miRNA processing disruption and PTEN upregulation.

Conclusions:

  • AP1 is a promising novel Pt(IV) prodrug targeting APE1 and the BER pathway.
  • AP1 effectively inhibits cancer cell growth, including cisplatin-resistant types, with a favorable safety profile.
  • The findings highlight the therapeutic potential of targeting BER via APE1 inhibition for enhanced cancer treatment.