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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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Phase II Reactions: Methylation Reactions01:17

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Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
The mechanism of methylation unfolds in two stages. The first stage sees a methyltransferase enzyme facilitating the transfer of a methyl group from S-adenosylmethionine (SAM) to the substrate, forming S-adenosylhomocysteine (SAH). The second stage involves further metabolism of SAH into homocysteine, which can be recycled...
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Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

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Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
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Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

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Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
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Spreading of Chromatin Modifications02:25

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The histone proteins in the nucleosomes are post-translationally modified (PTM) to increase or decrease access to DNA. The commonly observed PTMs are methylation, acetylation, phosphorylation, and ubiquitination of lysine amino acids in the histone H3 tail region. These histone modifications have specific meaning for the cell. Hence, they are called "histone code". The protein complex involved in histone modification is termed as "reader-writer" complex.
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Updated: Jul 15, 2025

Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays
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KDM4 Demethylases: Structure, Function, and Inhibitors.

Yuanyuan Jiang1, Lanxin Liu1, Zeng-Quan Yang2

  • 1Department of Oncology, Karmanos Cancer Institute, Wayne State University, 4100 John R Street, HWCRC 815, Detroit, MI, 48201, USA.

Advances in Experimental Medicine and Biology
|September 26, 2023
PubMed
Summary
This summary is machine-generated.

KDM4 histone demethylases regulate gene expression and are implicated in cancer. This review covers KDM4 protein structure, regulation, roles in pathology, and potential therapeutic inhibitors for cancer treatment.

Keywords:
CancerHistone demethylaseInhibitorsKDM4

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Area of Science:

  • Biochemistry
  • Epigenetics
  • Molecular Biology

Background:

  • KDM4 histone demethylases remove methyl marks from H3K9 and H3K36, regulating chromatin structure and gene expression.
  • These enzymes are crucial for transcription, cell proliferation, differentiation, DNA repair, immune response, and stem cell renewal.
  • Dysregulated KDM4 expression is linked to various blood and solid tumors, highlighting their therapeutic potential.

Purpose of the Study:

  • To summarize current knowledge on KDM4 protein structures and regulatory mechanisms.
  • To review the alterations of KDM4 proteins in human pathological processes, particularly in development and cancer.
  • To discuss KDM4 inhibitors as potential therapeutic agents.

Main Methods:

  • Literature review of KDM4 histone demethylases.
  • Analysis of KDM4 protein structures and regulatory pathways.
  • Examination of KDM4 involvement in pathological conditions and cancer.

Main Results:

  • KDM4 demethylases play critical roles in fundamental biological processes.
  • Aberrant KDM4 expression is a hallmark of numerous cancers.
  • Various KDM4 inhibitors have been developed and show therapeutic promise.

Conclusions:

  • KDM4 proteins are key epigenetic regulators with significant implications in cancer.
  • Understanding KDM4 structure and regulation is vital for developing targeted therapies.
  • KDM4 inhibitors represent a promising strategy for cancer treatment.