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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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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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Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
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Related Experiment Video

Updated: Nov 1, 2025

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Fragment-Derived Selective Inhibitors of Dual-Specificity Kinases DYRK1A and DYRK1B.

David Lee Walmsley1, James B Murray1, Pawel Dokurno1

  • 1Vernalis (R&D) Ltd., Granta Park, Cambridge CB21 6GB, U.K.

Journal of Medicinal Chemistry
|June 18, 2021
PubMed
Summary
This summary is machine-generated.

Researchers developed a selective DYRK1A inhibitor for potential cancer and Down's syndrome therapies. This brain-penetrant compound demonstrated in vivo activity in a tumor model, offering a new tool for disease research.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • DYRK1A kinase regulates key cellular processes in cancer, including cell cycle, DNA repair, apoptosis, differentiation, and metastasis.
  • Elevated DYRK1A activity correlates with increased symptom severity in Down's syndrome.
  • Targeting DYRK1A offers potential therapeutic benefits for cancer and neurological disorders.

Purpose of the Study:

  • To discover and characterize a selective inhibitor of DYRK1A.
  • To evaluate the inhibitor's properties, including selectivity, tolerability, and brain penetration.
  • To assess the in vivo efficacy of the DYRK1A inhibitor in a disease model.

Main Methods:

  • Employed fragment and structure-based drug discovery approaches.
  • Utilized in vitro assays to confirm selectivity and tolerability.
  • Tested the inhibitor's efficacy in an in vivo tumor model.

Main Results:

  • Identified a highly selective DYRK1A inhibitor.
  • The inhibitor was well-tolerated and demonstrated brain penetration.
  • In vivo studies showed activity in a tumor model, confirming therapeutic potential.

Conclusions:

  • A novel, selective, brain-penetrant DYRK1A inhibitor was successfully developed.
  • This compound serves as a valuable tool for studying DYRK1A's role in disease.
  • Further research into DYRK1A inhibition is warranted for therapeutic applications.