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Related Concept Videos

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.
There are several types of targeted therapies against...
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Targets for Drug Action: Overview01:26

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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
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Hormones intricately bind to receptors on the surface or within target cells, initiating a cascade of cellular responses.
Notably, the cellular response can be regulated by altering the number of receptors expressed in the cell. For example, prolonged exposure to elevated hormone levels results in a gradual decline or down-regulation in the number of receptors for that specific hormone on the cell surface. Conversely, in response to low hormone levels, cells may use up-regulation, producing an...
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Digestion begins with a cephalic phase that prepares the digestive system to receive food. When our brain processes visual or olfactory information about food, it triggers impulses in the cranial nerves innervating the salivary glands and stomach to prepare for food.
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In cross-sectional research, a researcher compares multiple segments of the population at the same time. If they were interested in people's dietary habits, the researcher might directly compare different groups of people by age. Instead of following a group of people for 20 years to see how their dietary habits changed from decade to decade, the researcher would study a group of 20-year-old individuals and compare them to a group of 30-year-old individuals and a group of 40-year-old...
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Plant hormones—or phytohormones—are chemical molecules that modulate one or more physiological processes of a plant. In animals, hormones are often produced in specific glands and circulated via the circulatory system. However, plants lack hormone-producing glands.
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Related Experiment Video

Updated: Jan 24, 2026

Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays
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Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays

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A chemoprobe tracks its target.

Aseem Z Ansari1

  • 1Department of Biochemistry, University of Wisconsin, Madison, Wisconsin 53706.

The Journal of Biological Chemistry
|May 19, 2019
PubMed
Summary

Researchers developed a new assay to directly measure small-molecule inhibitors binding to histone lysine demethylase KDM1A. This method offers a more accurate way to monitor these cancer drug candidates compared to indirect histone mark analysis.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Small-molecule inhibitors targeting histone-modifying enzymes are crucial in cancer therapy.
  • Current methods rely on indirect monitoring of histone marks, which can be unreliable due to enzyme redundancy.
  • Accurate assessment of inhibitor engagement is vital for drug development.

Purpose of the Study:

  • To develop a direct assay for monitoring inhibitor binding to histone-modifying enzymes.
  • To specifically validate this assay for the histone lysine demethylase KDM1A.
  • To provide a more reliable method for assessing the efficacy of potential cancer therapeutics.

Main Methods:

  • Development of a luminescence-based ELISA (Enzyme-Linked Immunosorbent Assay).
  • Directly measures the binding of small-molecule inhibitors to KDM1A.

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  • Utilizes KDM1A as the target for inhibitor screening and validation.

    • Main Results:

    • The developed ELISA successfully and directly monitors the binding of inhibitors to KDM1A.
    • This assay provides a more precise readout of inhibitor engagement than indirect histone mark assays.
    • Demonstrates the utility of a direct binding assay for epigenetic drug discovery.

    Conclusions:

    • A novel luminescence-based ELISA enables direct measurement of KDM1A inhibitor binding.
    • This direct assay overcomes limitations of indirect monitoring, improving reliability in drug discovery.
    • The method holds promise for advancing the development of epigenetic therapies for diseases like cancer.