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Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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M-Cdk Drives Transition Into Mitosis02:15

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Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
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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.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
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The JAK-STAT Signaling Pathway01:20

The JAK-STAT Signaling Pathway

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Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as  SH2...
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PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

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The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a...
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Updated: May 7, 2026

A Combined 3D Tissue Engineered In Vitro/In Silico Lung Tumor Model for Predicting Drug Effectiveness in Specific Mutational Backgrounds
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Protein Kinase Inhibitors: Synthesis and Molecular Repurposing in Three-Dimensional Cancer Models PKI.

Vladislav Lobanov1, Natalia Rossomakhina1, Elena Kazakova1

  • 1Research Centre of Biotechnology RAS, Moscow, Russia.

Chemical Biology & Drug Design
|November 6, 2025
PubMed
Summary

Molecular repurposing and 3D organoids offer new strategies to overcome drug resistance in cancer. These approaches target specific cancer tissues, improving therapeutic effectiveness against resistant tumors.

Keywords:
3D tissuedrug screeningmolecular repurposingorganoidsprecision medicineprotein kinase inhibitorstargeted drugstumoroids

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Area of Science:

  • Oncology
  • Pharmacology
  • Biotechnology

Background:

  • Targeted cancer therapies face challenges like treatment resistance and drug toxicity.
  • Developing new therapeutic molecules is costly and time-consuming.

Purpose of the Study:

  • To review protein kinase inhibitors, their synthesis, and mechanisms of action.
  • To explore molecular drug repurposing and 3D organoid models for cancer therapy.
  • To highlight strategies for overcoming targeted drug resistance.

Main Methods:

  • Literature review of protein kinase inhibitors and their approved drugs.
  • Analysis of molecular drug repurposing strategies.
  • Examination of 3D tissue-specific organoid (tumoroid) modeling for drug screening.

Main Results:

  • Protein kinase inhibitors are a key focus in targeted cancer therapy.
  • Molecular repurposing offers a viable strategy to utilize existing drugs for new targets.
  • 3D organoids show promise as a platform for screening anticancer agents, including protein kinase inhibitors.

Conclusions:

  • Molecular drug repurposing and advanced 3D organoid models are crucial for developing effective cancer treatments.
  • These strategies are vital in combating resistance to targeted therapies.
  • Personalized treatment approaches considering tissue-specific characteristics are essential.