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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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Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
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Tumor progression is a phenomenon where the pre-formed tumor acquires successive mutations to become clinically more aggressive and malignant. In the 1950s, Foulds first described the stepwise progression of cancer cells through successive stages.
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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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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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Antitumour Anthracyclines: Progress and Perspectives.

Maristela B Martins-Teixeira1, Ivone Carvalho1

  • 1School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo Avenida do Café s/n Monte Alegre, Ribeirão Preto, 14040903, Brazil.

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|April 22, 2020
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Summary

Anthracyclines are effective cancer drugs, but resistance and cardiotoxicity limit their use. This review examines anthracycline analogues, focusing on structural changes impacting efficacy and safety.

Keywords:
cardiotoxicitydoxorubicindrug discoverymultidrug resistancetopoisomerases

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Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Oncology

Background:

  • Anthracyclines are potent anticancer agents acting via DNA intercalation, oxidative stress, and topoisomerase II inhibition.
  • Key limitations include multidrug resistance and severe cardiotoxicity, driving the need for novel analogues.

Purpose of the Study:

  • To review clinically relevant anthracyclines and their developmental history.
  • To analyze the impact of structural modifications on antitumour activity, toxicity, and resistance profiles.

Main Methods:

  • Comprehensive literature review of anthracycline development.
  • Analysis of preclinical and clinical data for registered drugs, candidates, and investigational compounds.

Main Results:

  • Detailed overview of natural prototypes, semisynthetic, and synthetic anthracycline derivatives.
  • Exploration of structure-activity relationships influencing efficacy and safety.

Conclusions:

  • Structural modifications are crucial for overcoming anthracycline resistance and reducing cardiotoxicity.
  • Ongoing research aims to develop safer and more effective anthracycline-based cancer therapies.